Artículos de revistas: "Hydrazene"

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Ibtehal K. Abdullah y Meaad K. Buniya. "Preparation and Identification of some heterocyclic compounds from cyano compounds". Tikrit Journal of Pure Science 20, n.º 5 (10 de febrero de 2023): 96–105. http://dx.doi.org/10.25130/tjps.v20i5.1245.

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This article included prepared cyano acetic acid hydrazid from interaction cyano ethylacetate with hydrate hydrazen, and interaction with 2- acytel thiophene and 2- acytelpyridine it will formation of hydrazide- hydrazone derivative (I, II), and through the undergo the compounds (I,II) for chain of interactions with different chemical materials then enclosed cyclo formed derivative of (arylidene ,coumarin , aryl hydrazon , thiophene ) . Prepared compounds have been studied and Identification by physical and spectral means.

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Ekram Abdullah Basheer, Kalid Matny Al-jaanaby y Feras Shauki Al-joboury. "Synthesis a Number of Heterocyclic Compounds Derived From Levofloxacin". Tikrit Journal of Pure Science 20, n.º 5 (10 de febrero de 2023): 84–95. http://dx.doi.org/10.25130/tjps.v20i5.1244.

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In this paper, the preparation a number of heterocyclic compounds five membered rings like oxadiazole, imidazolidine, thiozolidine, tetrazole, azetidine 2-on. Hydrazide (1) was synthesized from the reaction of levofloxacin with hydrazine hydrate. Hydrazone compounds (2-9) were synthesized from the reaction (1) with a number of aldehydes, and 3-acetyl-1,3,4-oxadiazol (10-17) was prepared from the reaction of hydrazones (2-9) with acetic anhydride, 5-oxo-2-aryl imadazoldine derivative (18-25) were prepared from the reaction of hydrazone derivatives (2-9) with glycine, while the reaction of hydrazone with thioglygolic acid gave 4-oxo-2-aryl-thiozolidine (26-33),tetrazole derivative(34-41)prepared from the reaction of hydrazone(2-9) with sodium azide in tetrahyro furan.azetidine-2-on(42-49)with chloro acetyl chloride in DMF and and in the presence of triethyl amine these compounds were characterized on bases of spectral and physical data.

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Agili, Fatimah. "Novel Hydrazide Hydrazone Derivatives as Antimicrobial Agents: Design, Synthesis, and Molecular Dynamics". Processes 12, n.º 6 (22 de mayo de 2024): 1055. http://dx.doi.org/10.3390/pr12061055.

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Ester 2 was produced by reacting thiourea derivative 1 with ethyl 2-chloro-3-oxobutanoate in MeOH containing piperidine. Hydrazide 3 was produced by reacting the latter ester with hydrazine hydrate in EtOH at reflux. By reacting hydrazide 3 with aromatic/heterocyclic aldehydes, twelve derivatives of hydrazide hydrazone 5a–l were produced. Spectral measurements and elemental analysis verified the molecular structure. Compounds 2, 5a, 5c, 5d, and 5f had strong effects on all the pathogenic bacterial strains according to an evaluation of the antimicrobial qualities of the synthetic compounds. With inhibitory zone diameters ranging from 16 to 20.4 mm, hydrazide hydrazone 5f exhibited the strongest activity. Additionally, the minimum inhibitory concentration (MIC) was assessed. The best outcomes were found with hydrazones 5c and 5f. For B. subtilis, the MIC of 5c was 2.5 mg/mL. For E. coli and K. pneumoniae, the MIC of 5f was 2.5 mg/mL. The molecular mechanics-generalized born surface area (MM/GBSA) was utilized to compute binding free energies via a molecular dynamics simulation analysis of the most active compounds, 5f and 5c. Moreover, computational analyses demonstrated that 5f had a substantial affinity for the active site of DNA gyrase B, suggesting that this compound could be a strong platform for new structure-based design efforts.

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Kaur, Aneet Kamal, Renu Bala, Poonam Kumari, Sumit Sood y Karan Singh. "Microwave Assisted Vilsmeier-Haack Reaction on Substituted Cyclohexanone Hydrazones: Synthesis of Novel 4,5,6,7-Tetrahydroindazole Derivatives". Letters in Organic Chemistry 16, n.º 3 (11 de febrero de 2019): 170–75. http://dx.doi.org/10.2174/1570178615666180917101637.

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Vilsmeier-Haack reaction is one of the most important chemical reactions used for formylation of electron-rich arens. Even though Vilsmeier-Haack reaction was studied on a wide variety of hydrazones of enolizable ketones, literature lacks the examples of the use of 4-substituted cyclohexanones as a substrate. The cyclization potential of hydrazones of cyclic keto compounds is still interested topic of investigation. In the present study, the reaction of various hydrazines with 4-substituted cyclohexanones was proceeded and the resulted hydrazones in crude form were treated with Vilsmeier- Haack reagent using both conventional as well as microwave methods. The reaction of phenyl hydrazine with 4-phenylcyclohexanone yielded the corresponding tetrahydro-1H-carbazole instead of hydrazone during solvent evaporation at 40ºC. By keeping the temperature of water bath to 0ºC, the corresponding hydrazone was isolated in crude form which was immediate treated with POCl3/DMF for 10 min at 90ºC using microwave irradiation method afforded novel 4,5,6,7-tetrahydroindazole derivative. Using this optimized condition, the substrate scope for the synthesis of tetrahydroindazole derivatives was explored and synthesized total 6 final compounds. The microwave assisted synthesis of tetrahydroindazoles from 4-substituted cyclohexanones has been reported for the first time under mild conditions in good yield. Easy work up procedure, high yielding, shortened reaction times, clean and ecofriendly are the main advantages of this protocol.

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5

Prateeptongkum, Saisuree, Nongnaphat Duangdee y Wiratchanee Mahavorasirikul. "Evaluation of Cytotoxicity and Apoptosis Induced by Coumarin Hydrazide-Hydrazone Derivatives in Human Hepatocellular Carcinoma Cell Line". Trends in Sciences 21, n.º 7 (1 de mayo de 2024): 7628. http://dx.doi.org/10.48048/tis.2024.7628.

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Coumarin and aryl hydrazide-hydrazone have attracted our attention due to their vast biological properties. Previous studies suggested that coumarin-tethered aryl hydrazide-hydrazone showed potent activities against HepG2. In the present study, we investigated the cytotoxic potency of the coumarin derivatives 1 - 3 to compare with coumarin hydrazine-hydrazone hybrids 4 and 5 against hepatocellular carcinoma HepG2 and LH86 cell lines. Among the tested coumarins, hybrids 4 and 5 showed highly potent activity against HepG2 with IC50 values of 17.82 ± 2.79 and 7.87 ± 0.88 𝜇g/mL, respectively. The hybrid 4 also showed the strongest activity against LH86 cell line with IC50 values of 48.32 ± 2.64 𝜇g/mL. Further, we have studied the mechanism of action of the hybrid compounds 4 and 5 in HepG2 cells via the flow-cytometry analysis and the activation of the caspase-3 and caspase-7. The results showed that hybrids 4 and 5 obviously inhibited the proliferation of HepG2 cell line through inducing apoptosis. HIGHLIGHTS Focusing on coumarin and aryl hydrazide-hydrazone possess significant biological properties. We reported the preparation of coumarin hydrazine-hydrazone hybrids and evaluated their effects against hepatocellular carcinoma cell lines HepG2 and LH86. The hybrid compounds exhibited high potency against HepG2 and LH86. Flow-cytometry and caspase-3/7 expression analysis revealed that the hybrid compounds induced apoptosis in HepG2 cells. GRAPHICAL ABSTRACT

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Alheety, Nuaman. "Synthesis, Characterization and Antimicrobial Activity Study of Some New Substituted Benzoxazole Derivatives". Baghdad Science Journal 16, n.º 3 (1 de septiembre de 2019): 616. http://dx.doi.org/10.21123/bsj.2019.16.3.616.

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This research included the preparation of 2-mercaptobenzoxazole (N1) by the reaction of ortho-aminophenol with carbon disulfide in an alcoholic potassium hydroxide solution. The 2-mercapto benzoxazole (N1) was then treated with hydrazine to obtain the 2-hydrazino benzoxazole (N2). A number of hydrazones (N3-N5) were prepared through the reaction of N2 with different benzaldehydes. The compound (N6) was also prepared whereby the ring closing of hydrazone (N3) using chloroacetylchloride, while the compound (N7) was prepared by treating 2-hydrazino benzoxazole with acetylacetone. When the compound (N1) was treated with formaldehyde, it afforded the compound (N8). Also, the N9 was obtained from the reaction of N1 with chloroacetic acid in the presence of alcoholic potassium hydroxide. The prepared compounds were characterized using physico-chemical and spectroscopic methods such as melting point, infrared spectroscopy (IR) and the proton nuclear magnetic resonance (1H-NMR). Thereafter, some of the compounds were selected for in vitro antibacterial activity and one of these compounds showed an inhibition effect against gram positive only which is very important because it is considered as specific antibacterial drug.

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7

Popiołek, Łukasz. "Updated Information on Antimicrobial Activity of Hydrazide–Hydrazones". International Journal of Molecular Sciences 22, n.º 17 (30 de agosto de 2021): 9389. http://dx.doi.org/10.3390/ijms22179389.

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Hydrazide–hydrazones possess a wide spectrum of bioactivity, including antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antidepressant, antiviral, and antiprotozoal properties. This review is focused on the latest scientific reports regarding antibacterial, antimycobacterial, and antifungal activities of hydrazide–hydrazones published between 2017 and 2021. The molecules and their chemical structures presented in this article are the most active derivatives, with discussed activities having a hydrazide–hydrazone moiety as the main scaffold or as a side chain. Presented information constitute a concise summary, which may be used as a practical guide for further design of new molecules with antimicrobial activity.

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8

Al-Shiekh, Mariam A., Hanady Y. Medrassi, Mohamed H. Elnagdi y Ebtisam A. Hafez. "Substituted Hydrazonals as Building Blocks in Heterocyclic Synthesis: A New Route to Arylhydrazonocinnolines". Journal of Chemical Research 2007, n.º 7 (julio de 2007): 432–36. http://dx.doi.org/10.3184/030823407x234617.

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2-heteroylhydrazonopropanals 2a–e and 3-oxo-2-arylhydrazonopropanals 2f–k were prepared via coupling of enaminones 1 with aromatic diazonium salts. Compounds 2a–c condensed with hydrazine hydrate to yield the corresponding hydrazones 3a–c which afford on cyclisation the cinnoline derivatives 6a–c, while condensation of 2g, j with hydrazine hydrate directly yielded the pyrazole derivatives 4g–j. Condensation of 2a–c, f, g with phenyl hydrazine gave the corresponding phenyl hydrazone derivatives 7a–c, f, g. Structures of 2a, h and 3a were assessed by single crystal X-ray analyses.

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9

Avdeenko, A. P., S. A. Konovalova, I. Yu Yakymenko, V. M. Baumer, S. V. Shishkina y V. V. Pirozhenko. "Interaction of 4-{[(tolyl(methane)sulphonyl)oxy]imino}cyclohexa-2,5-dien-1-ones with N-nucleophiles". Voprosy Khimii i Khimicheskoi Tekhnologii, n.º 1 (enero de 2021): 3–11. http://dx.doi.org/10.32434/0321-4095-2021-134-1-3-11.

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Hydrazones of 1,4-benzoquinone, which have a wide range of biological activities, can be synthesized in the reactions of 4-{[(arylsulfonyl)oxy]imino}cyclohexa-2,5-diene-1-ones or N-(4-oxocyclohexa-2,5-diene-1-ylidene)arylsulfonamides with N-substituted hydrazines. In this study, the reaction of 2,6-disubstituted 4-{[(tolyl(methane)sulfonyl)oxy]imino}cyclohexa-2,5-diene-1-ones with aroylhydrazides gave N'-(3,5-dialkyl-4-oxocyclohexa-2,5-diene-1-ylidene)aroylhydrazides, which can be obtained by cross-synthesis in the reaction of N-(3,5-dialkyl-4-oxocyclohexa-2,5-dien-1-ylidene)arylsulfonamides with aroylhydrazides. As a result of the reaction of 4-{[(tolyl(methane)sulfonyl)oxy]imino}cyclohexa-2,5-dien-1-ones with phenylhydrazine, stable 4-hydroxyanilinium tolyl(methane)sulfates were isolated. Their structures were confirmed by X-ray diffraction data. We suggested that at the first stage of the reaction between 4-{[(tolyl(methane)sulfonyl)oxy]imino}cyclohexa-2,5-diene-1-ones and hydrazines, the N–O bond of starting 4-(oxyimino)cyclohexa-2,5-diene-1-one was broken forming sulfonic acid and corresponding quinoneimine. The latter either can be reduced to corresponding aminophenol under reaction conditions or can react with an excess of N-substituted hydrazine yielding corresponding hydrazide. The formation of N'-(4-oxocyclohexa-2,5-diene-1-ylidene)arohydrazides is facilitated by a lower basicity of hydrazide and a lower redox potential of quinoneimine.

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10

Wu, Shouting, Xi Liang, Fang Luo, Hua Liu, Lingyi Shen, Xianjiong Yang, Yali Huang et al. "Synthesis, Crystal Structure and Bioactivity of Phenazine-1-carboxylic Acylhydrazone Derivatives". Molecules 26, n.º 17 (1 de septiembre de 2021): 5320. http://dx.doi.org/10.3390/molecules26175320.

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A phenazine-1-carboxylic acid intermediate was synthesized from the reaction of aniline and 2-bromo-3-nitro-benzoic acid. It was then esterified and reacted with hydrazine hydrate to afford phenazine-1-carboxylic hydrazine. Finally, 10 new hydrazone compounds 3a–3j were obtained by the condensation reaction of phenazine-1-carboxylic acid hydrazide and the respective aldehyde-containing compound. The structures were characterized by 1H and 13C NMR spectroscopy, MS and single crystal X-ray diffraction. The antitumor activity of the target compounds in vitro (HeLa and A549) was determined by thiazolyl blue tetrazolium bromide. The results showed that compound (E)-N′-(2-hydroxy-4-(2-(piperidine-1-yl) ethoxy) benzyl) phenazine-1-carbonyl hydrazide 3d exhibited good cytotoxic activity.

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11

Geschwentner, Michael, Gernot Elter y Anton Meller. "Supermesityl-substituierte Hydrazinoborane / Supermesityl-Substituted Hydrazinoboranes". Zeitschrift für Naturforschung B 49, n.º 4 (1 de abril de 1994): 459–64. http://dx.doi.org/10.1515/znb-1994-0405.

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Difluoro(supermesityl)borane reacts with monolithiated hydrazines to give the correspond ing fluoroborylated hydrazines 1a-c , which could not be dehydrofluorinated to yield definite products. From dilithiated hydrazine the 1,2-borylated species 2 was obtained. The fluoro-borylhydrazones 3a-3d prepared in an analogous way, by dehydrofluorination with tert-butyllithium, led to 5-, 6-and 7-membered boron nitrogen heterocycles depending upon the substituents of the hydrazones.

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12

Shu, Zhang, Wang Longyu, Cao Pengzhang, Gu Xuefan, Zhang Huani y Chen Gang. "Synthesis of New Hydrazone Compounds from Natural Grease and Investigation as Flow Improver for Crude Oil". Нефтехимия 63, n.º 3 (15 de junio de 2023): 354–62. http://dx.doi.org/10.31857/s0028242123030061.

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n this work, salicylaldehyde hydrazone (SAH), different from the traditional polymers, was synthesized from natural oils (castor, SAСH, rapeseed, SARH and soybean, SASH), hydrazine hydrate and salicylaldehyde. Firstly, natural grease reacts with hydrazine hydrate to produce hydrazide, and then salicylaldehyde reacts with hydrazide to synthesis salicylaldehyde hydrazone. In this work, SAH were evaluated as viscosity-reducers and pour point depressors for crude oil. The results show that the SAH can significantly reduce the pour point and viscosity of crude oil, with the increase of crude oil fluidity, the viscosity reduction rate of сrude oil from Jinghe Oilfield (QHO) reaches to 80.1% (40°С), the pour point decreases by 12.1°С, the viscosity reduction rate of сrude oil from Xinjiang Oilfield (STO) reaches to 87.5% (15°С), and the pour point decreases by 6.2°С. Based on the efficiency of different SAH, structure-function relationship was discussed. The mechanism of SAH effecting on crude oil is that the long alkyl chain is conducive to inhibiting the growth of crystals when eutectic with wax nuclei in heavy oil, and plays the role of pour point and viscosity reduction.

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13

Nocheva, Hristina, Stanislava Vladimirova, Diana Tzankova, Lily Peikova y Maya Georgieva. "Analgesic properties of newly synthesized N pyrrolyl hydrazide hydrazones". Tropical Journal of Pharmaceutical Research 22, n.º 1 (18 de febrero de 2023): 121–27. http://dx.doi.org/10.4314/tjpr.v22i1.17.

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Purpose: To screen a series of newly synthesized N-pyrrolyl hydrazide hydrazones for analgesic activity via Paw-pressure (PP) test and hot plate test (HPT). Methods: The compounds newly synthesized through the classical Paal-Knor cyclization, N-pyrrolyl hydrazide-hydrazones were administered intraperitoneally at a dose of 20 mg/kg. Paw pressure and hot plate tests were applied to assess the analgesic properties. In addition, stress-induced analgesia with naloxone as a non-selective opioid receptor antagonist was performed. Results: The compound (DI-5g), containing an izatine carbonyl fragment, was the most promising. It presented the highest paw pressure threshold (25 AU at 30th min) by exceeding the analgesic activity of the referent metamizole (23 AU at 30th min). The relative effect from the hot plate test was consistent with the paw pressure results. Opioid receptors were involved in the analgesic activities of N-pyrrolyl hydrazide-hydrazones. Conclusion: The N-pyrrolyl carboxylic acids are synthesized and identified as new compounds and their hydrazide-hydrazone derivatives as promising leads for future design and synthesis of drugs with possibly prolonged analgesic activity.

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Abdelmohsen, Shawkat A. y Talaat I. El Emary. "SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF NOVEL PYRAZOLO[3,4-b]PYRIDINES AND THEIR SPIRO-HETEROCYCLIC DERIVATIVES". JOURNAL OF ADVANCES IN CHEMISTRY 10, n.º 7 (22 de enero de 2014): 2901–15. http://dx.doi.org/10.24297/jac.v10i7.6802.

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The present work describes the synthesis of a novel series of heterocyclic moieties derived from 5-acetylpyrazolo[3,4-b]pyridine (1). The formation of chalcones (2a-d) was utilized to synthesize pyrazoline, isoxazoline and pyrimidine derivatives (3-10). Thiosemicarbazone and semicarbazone (11, 17) were utilized to synthesize other new triazolethiones, thiadiazole and selenadiazole derivatives (11-19). Some new spiro derivatives (22-25) were synthesized by the reaction of chalcone (21) of 1 and isatine with hydrazines, hydroxyl amines and thiourea. Also, The reaction of 1 with cyanoacetyl hydrazine gave the hydrazide-hydrazone derivative 26, which was allowed to react with aromatic aldehydes and α-cyanocinnamonitrile to afford coumarine and substituted pyridine derivatives (28, 29). The structures of all the new compounds have been established on the basis of their analytical and spectral data. Twenty two of the synthesized compounds were also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi and most are found to possess promising antimicrobial activity when compared with Chloramphenicol and Clotrimazole

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15

Hrnčiar, Pavel y Eva Švanygová. "Reactions of 2-Acyl-1,3-indandiones with Nitrogen Nucleophiles". Collection of Czechoslovak Chemical Communications 59, n.º 12 (1994): 2734–40. http://dx.doi.org/10.1135/cccc19942734.

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Reactions of 2-acyl-1,3-indandiones with nitrogen nucleophiles were studied rarely. The question, if they react with carbonyl carbon of acyl group or indandione skeleton, has not been answered unambiguously. To make clear the question which carbonyl carbon of 2-acyl-1,3-indandiones enters the reaction with nitrogen nucleophiles we carried out the reactions with 2-acetyl- (Ia), 2-propionyl- (Ib), 2-pivaloyl- (Ic), and 2-benzoyl-1,3-indandione (Id). We used different 2-acyl-1,3-indandiones with the aim to find out if the character of acyl group affects the course of reaction. We used ethoxyamine, primary amines, phenylhydrazine, hydrazine and methylhydrazine as nucleophile reactants. The reactions were carried out in methanol at reflux at 10% excess of nitrogen base. The reactions with phenylhydrazine, hydrazine and methylhydrazine were performed with twofold excess of nitrogen base. The separation of reaction products was carried out by chromatography on silica gel. We found that 2-acyl-1,3-indandiones I react with ethoxyamine both at the acylcarbonyl carbon to produce 2-(1-ethoxyiminoalkyl)-1,3-indandiones II and the carbonyl carbon of indandione skeleton to give rise 3-(ethoxyimino)-2-acyl-1-indanones III. In all cases, the carbonyl carbon of acyl group was preferred (the observed ratio of products II to III was 6 - 8 : 1). From the reaction of 2-acyl-1,3-indandiones with primary amines only the products IV of reaction with the acylcarbonyl carbon were isolated. The hydrazines used reacted with 2-acyl-1,3-indandiones also at carbonyl carbon of acyl group in the first step to produce hydrazones. However, the products isolated in most cases were formed by the attack of hydrazone nitrogen at carbonyl carbon of indandione skeleton giving rise to derivatives of indeno[2,3-d]pyrazole-4-one V. It is interesting that 2-acetyl-1,3-indandione and 2-propionyl-1,3-indandione, reacting with phenylhydrazine and hydrazine, yielded only corresponding hydrazones VI.

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16

Agarwal, Mahadev, Neelam Singla y S. K. Singh. "Novel Synthesis, Physicochemical Characterization of 1,3,4-Oxadiazinoindole Derivatives for the Purpose of Antidepressant Activity". INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 13, n.º 03 (25 de septiembre de 2023): 936–41. http://dx.doi.org/10.25258/ijddt.13.3.26.

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The present study synthesized a series of 1,3,4-oxadiazinoindole moiety-containing compounds by combining MAOI’s hydrazide moiety and tricyclic moiety having antidepressant activity. The formation of amino acid chloride from amino acids started the synthesis. Further, they were converted into amino acid hydrazide, and then amino acid hydrazones were prepared by reaction of amino acid hydrazide with isatin. Finally, cyclization was acted on hydrazone-containing compounds in the presence of cold H2SO4. Synthesized compounds are characterized and confirmed via mass spectroscopy, 1H-nuclear magnetic resonance strategies, fourier transform infrared spectroscopy, thin layer chromatography, and melting point. The compounds were evaluated for antidepressant activity.

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17

Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds". Journal of Chemical Research 37, n.º 1 (enero de 2013): 6–10. http://dx.doi.org/10.3184/174751912x13543818811749.

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Synthesis of a new 4-hydrazinopyrazolo[3,4- d]pyrimidine was achieved via heating (4,6-dithioxo-1 H-pyrazolo[3,4- d] pyrimidin-3-yl)acetonitrile with hydrazine hydrate. Reactions of the latter product with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues afforded the corresponding hydrazone and pyrazole derivatives, respectively. Similarly, condensation of 2-[6-(benzylsulfanyl)-4-hydrazino-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues gave the respective hydrazone and pyrazolone derivatives. Alkylation reactions of 2-[4,6-bis(benzylsulfanyl)-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with arylamines gave the respective 4-( N-arylamino)-6-benzylsulfanylpyrazolo[3,4- d]pyrimidine derivatives.

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18

Lerner, Hans-Wolfram, Nils Wiberg, Michael Bolte, H. Nöth y J. Knizek. "Supersilyliertes Ammoniak und supersilyliertes Hydrazin: Synthese, Struktur und Eigenschaften / Supersilyl Ammonia and Supersilyl Hydrazine: Synthesis, Structure and Properties". Zeitschrift für Naturforschung B 57, n.º 2 (1 de febrero de 2002): 177–82. http://dx.doi.org/10.1515/znb-2002-0208.

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An excellent supersilylation agent, supersilyl triflate, tBu3SiO3SCF3, is easily obtained from tBu3SiH and CF3SO3H. Supersilyl triflate, tBu3SiO3SCF3, reacts with lithium amide or lithium hydrazide to form the supersilyl amine, tBu3SiNH2, or the supersilyl hydrazines, tBu3SiNHNH2 and tBu3SiNH-HNSitBu3, respectively. The structures of supersilyl triflate, tBu3SiO3SCF3, and bissupersilyl hydrazine, tBu3SiNH-HNSitBu3, have been determined by X-ray structure analysis.

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19

Ienascu, Ioana M. c., Alfa X. Lupea, Iuliana M. Popescu, Stefan Th Tomas y Alina D. Zamfir. "Synthesis and Characterization of Some New 2-Hydroxy-N-(3-Trifluoromethyl-Phenyl)-Benzamide Derivatives". Revista de Chimie 59, n.º 1 (9 de febrero de 2008): 56–60. http://dx.doi.org/10.37358/rc.08.1.1707.

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In the reaction between 2-hydroxy-N-(3-trifluoromethyl-phenyl)-benzamide and chloro-acetic acid ethyl ester, [2-(3-trifluoromethyl-phenylcarbamoyl)-phenoxy]-acetic acid ethyl ester was obtained. The ethyl ester was condensed with hydrazine giving 2-hydrazinocarbonylmethoxy-N-(3-trifluoromethyl-phenyl)-benzamide. This hydrazide is considered the key intermediate for the synthesis of new compounds. So, in the reaction between hydrazide and chloro-substituted benzaldehydes hydrazones were obtained. In order to establish their structures, all new synthesized compounds were analyzed by modern physico-chemical methods (FTIR, 1H-NMR, 13C-NMR, MS).

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20

Gavara, Laurent, Federica Verdirosa, Alice Legru, Paola Sandra Mercuri, Lionel Nauton, Laurent Sevaille, Georges Feller et al. "4-(N-Alkyl- and -Acyl-amino)-1,2,4-triazole-3-thione Analogs as Metallo-β-Lactamase Inhibitors: Impact of 4-Linker on Potency and Spectrum of Inhibition". Biomolecules 10, n.º 8 (23 de julio de 2020): 1094. http://dx.doi.org/10.3390/biom10081094.

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To fight the increasingly worrying bacterial resistance to antibiotics, the discovery and development of new therapeutics is urgently needed. Here, we report on a new series of 1,2,4-triazole-3-thione compounds as inhibitors of metallo-β-lactamases (MBLs), which represent major resistance determinants to β-lactams, and especially carbapenems, in Gram-negative bacteria. These molecules are stable analogs of 4-amino-1,2,4-triazole-derived Schiff bases, where the hydrazone-like bond has been reduced (hydrazine series) or the 4-amino group has been acylated (hydrazide series); the synthesis and physicochemical properties thereof are described. The inhibitory potency was determined on the most clinically relevant acquired MBLs (IMP-, VIM-, and NDM-types subclass B1 MBLs). When compared with the previously reported hydrazone series, hydrazine but not hydrazide analogs showed similarly potent inhibitory activity on VIM-type enzymes, especially VIM-2 and VIM-4, with Ki values in the micromolar to submicromolar range. One of these showed broad-spectrum inhibition as it also significantly inhibited VIM-1 and NDM-1. Restoration of β-lactam activity in microbiological assays was observed for one selected compound. Finally, the binding to the VIM-2 active site was evaluated by isothermal titration calorimetry and a modeling study explored the effect of the linker structure on the mode of binding with this MBL.

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Krátký, Martin, Katarína Svrčková, Quynh Anh Vu, Šárka Štěpánková y Jarmila Vinšová. "Hydrazones of 4-(Trifluoromethyl)benzohydrazide as New Inhibitors of Acetyl- and Butyrylcholinesterase". Molecules 26, n.º 4 (13 de febrero de 2021): 989. http://dx.doi.org/10.3390/molecules26040989.

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Based on the broad spectrum of biological activity of hydrazide–hydrazones, trifluoromethyl compounds, and clinical usage of cholinesterase inhibitors, we investigated hydrazones obtained from 4-(trifluoromethyl)benzohydrazide and various benzaldehydes or aliphatic ketones as potential inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). They were evaluated using Ellman’s spectrophotometric method. The hydrazide–hydrazones produced a dual inhibition of both cholinesterase enzymes with IC50 values of 46.8–137.7 µM and 19.1–881.1 µM for AChE and BuChE, respectively. The majority of the compounds were stronger inhibitors of AChE; four of them (2-bromobenzaldehyde, 3-(trifluoromethyl)benzaldehyde, cyclohexanone, and camphor-based 2o, 2p, 3c, and 3d, respectively) produced a balanced inhibition of the enzymes and only 2-chloro/trifluoromethyl benzylidene derivatives 2d and 2q were found to be more potent inhibitors of BuChE. 4-(Trifluoromethyl)-N’-[4-(trifluoromethyl)benzylidene]benzohydrazide 2l produced the strongest inhibition of AChE via mixed-type inhibition determined experimentally. Structure–activity relationships were identified. The compounds fit physicochemical space for targeting central nervous systems with no apparent cytotoxicity for eukaryotic cell line together. The study provides new insights into this CF3-hydrazide–hydrazone scaffold.

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22

Gera, Ankur, Chander Mohan y Sandeep Arora. "Synthesis of Phthaloylglycyl Hydrazide Derivatives: Selective Protection of Phthalimide Group from Hydrazinolysis". Current Organic Synthesis 15, n.º 6 (29 de agosto de 2018): 839–45. http://dx.doi.org/10.2174/1570179415666180601083256.

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Background: N-phthalimide amino acid hydrazide is a class of compounds that have the potential therapeutic use. In general, hydrazinolysis of N-substituted amino acid(s) ester removes the ester group and yields the corresponding hydrazide. However, in case if N-substitution group is phthalimide, phthalimide group is cleaved and not the ester group. The resulted compound, therefore, is amino acid ester rather than Nphthalimide amino acid hydrazide. The above class of compounds, because of susceptibility of phthalimide group to hydrazinolysis, has previously been synthesized by a lengthy three-step procedure. Objective: N-phthaloylglycyl hydrazide was synthesized by using new efficient, simplified, one step process. Hydrazone derivatives from substituted benzaldehydes, and substituted furaldehyde were also synthesized. Method: N-phthaloylglycyl hydrazide was synthesized from the corresponding carboxylic acid using 1-Ethyl- 3-(3-dimethylaminopropyl)carbodiimide (EDC) as a coupling agent and hydroxybenzotriazole (HOBt) as an activator. Hydrazone derivatives were synthesized by condensation of N-phthaloylglycyl hydrazide with substituted benzaldehyde/substituted furaldehydes. All the compounds were characterized by IR, 1H-NMR, 13CNMR, mass spectroscopy and elemental analysis. Results: The presence of EDC/HOBt resulted in hydrazinolysis of the carboxylic acid group and not the phthalimide group. N-phthaloylglycyl hydrazide was synthesized in good yield. Conclusion: We report the improved process of the synthesis of N-phthaloylglycyl hydrazide. This is the first report where stability of phthaloyl amino acid compound to hydrazine is demonstrated. The reaction may be explored for the reaction schemes where stability of phthalimide group to hydrazinolysis is required.

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23

Assoma, Amon, Affoué Bede, Patrick-Armand Achi y Siomenan Coulibali. "Stability and Reactivity of Two Benzimidazole Hydrazide-Hydrazone Compounds: A Theoretical Study by DFT Method". International Journal of Computational and Theoretical Chemistry 12, n.º 1 (24 de mayo de 2024): 10–17. http://dx.doi.org/10.11648/j.ijctc.20241201.12.

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This work contributes to theoretical chemistry’s knowledge of benzimidazole-hydrazide-hydrazone. Indeed, hydrazides-hydrazones-benzimidazoles have shown anticancer, antibacterial, antiparasitic activities, and many other activities. A benzimidazole-hydrazide-hydrazone compound can exhibit four conformers: E/Z synperiplanar (Esp, Zsp) and E/Z antiperiplanar (Eap, Zap). Studies have indicated that the prevalence of these compounds is attributed to their stability and their tendency to readily bind to DNA. A theoretical study with advanced methods would make it possible to evaluate the stability of benzimidazole-hydrazide-hydrazone conformers. Therefore, we carried out this theoretical study on the conformers of two benzimidazoles-hydrazides-hydrazones denoted C1 and C2 wich differ by the presence of fluorine atom in the structure of C2. Specifically, we analyze the stability and the reactivity of the compounds based on the dipole moment, Gibbs free energy, HOMO and LUMO energies and UV-visible. For this purpose, calculations were performed in gas phase and DMSO using DFT and TD-DFT methods at the B3LYP/6-311+G(d, p) level theory. The dipole moment values show that Zap conformer is the most polar for both compounds. The Gibbs free energy indicate that Esp conformer emerges as the most stable for both compounds in both phases. The energy gap (ELUMO-EHOMO) and TD-DFT results suggest that Esp conformer is the most reactive conformer for the two compounds.

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24

Hossain, M. I. y M. M. H. Bhuiyan. "Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives". Journal of Scientific Research 1, n.º 2 (23 de abril de 2009): 317–25. http://dx.doi.org/10.3329/jsr.v1i2.2299.

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Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6 dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitrile 1 with formic acid, affording 5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one 2, which is chlorinated with thionyl chloride and then hydrazinated with hydrazine hydrate. Finally hydrazino compound 4 is reacted with formic acid, acetic anhydrate, benzaldehyde, p-hydroxybenzaldehyde, p-toluayldehyde, p-nitrobenzaldehyde and p-chlorobenzaldehyde to give thienotriazolopyrimidines 5-6 and thienopyrimidines 7-11 respectively. All the compounds have been screened for their antimicrobial activity. Keywords: Fused pyrimidines; Hydrazino compound; Thienotriazolopyrmidines; Thienopyrimidines; Antimicrobial activity.© 2009 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.DOI: 10.3329/jsr.v1i2.2299

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25

Ashry, El Sayed H. El, El Sayed Ramadan, Hamida Abdel Hamid y Mohamed Hagar. "Microwave Irradiation for Enhancing the Regioselective Synthesis of 6H-indolo[2,3-b]quinoxalines". Journal of Chemical Research 2005, n.º 4 (abril de 2005): 229–32. http://dx.doi.org/10.3184/0308234054213483.

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Microwave irradiation (MWI) promotes the regioselective synthesis of 6H-indolo[2,3-b] quin oxaline (5) by condensation of isatin (1) with o-phenylenediamine. Ethyl indolo [2,3-b] quinoxaline-6-acetate (8) was prepared via the carbethoxymethylation of 5, or from the reaction of N-(ethoxycarbonylmethyl)isatin (6) with o-phenylenediamine under MWI. The reaction of 8 with hydrazine hydrate afforded the hydrazide 9, whose condensation with aromatic aldehydes and monosaccharides gave the hydrazones 10a–d.

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26

Milyutin, Constantine Vyacheslavovich, Andrey Nikolaevich Komogortsev y Boris Valerievich Lichitsky. "Synthesis of 1,2,3-triazoles containing an allomaltol moiety from substituted pyrano[2,3-d]isoxazolones via base-promoted Boulton–Katritzky rearrangement". Beilstein Journal of Organic Chemistry 20 (11 de junio de 2024): 1334–40. http://dx.doi.org/10.3762/bjoc.20.117.

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For the first time, the interaction of aroyl containing pyrano[2,3-d]isoxazolone derivatives with various hydrazines was studied. It was shown that the considered process includes formation of corresponding hydrazones followed by Boulton–Katritzky rearrangement. As a result, the general method for the synthesis of substituted 1,2,3-triazoles bearing an allomaltol fragment was elaborated. The suggested approach can be applied to various aromatic and heterocyclic hydrazines. At the same time for unsubstituted hydrazine the Boulton–Katritzky recyclization is not implemented. In this case the opening of the pyranone ring was observed leading to pyrazolylisoxazole derivatives. Both types of aforementioned structures were proved by X-ray analysis.

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27

Groziak, Michael P. y Paul D. Robinson. "The Structural Basis for Hydrolysis Resistance in the Esters of (2-Formylphenyl)boronic Acid 2,4-Dinitrophenylhydrazones". Collection of Czechoslovak Chemical Communications 67, n.º 7 (2002): 1084–94. http://dx.doi.org/10.1135/cccc20021084.

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Under conditions that typically afford bicyclic boron heterocycles directly, (2-formylphenyl)boronic acids react with 2,4-dinitrophenylhydrazine in ethanol to give highly waterresistant diethyl boronate esters. Two such 2,4-dinitrophenylhydrazones were prepared and their X-ray crystal structures determined. Contrary to a previous suggestion that their unusual stability is due to an intramolecular N→B coordination giving a six-membered BN2C3 ring system based on a (Z)-hydrazone, these compounds instead were found to be (E)-hydrazones internally stabilized by a weak intramolecular interaction between nitrogen and boron from within a five-membered ring. Further study revealed that the electron deficiency of the starting hydrazine reagent plays a key role in determining the structure of the hydrazone isolated, and that the water-resistant boronate esters can be hydrolyzed under forcing conditions to the boronic acids.

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28

Abidov, Musa T. "Pharmacological aspects of hydrazides and hydrazide derivatives". Health Promotion & Physical Activity 2, n.º 3 (30 de junio de 2017): 9–21. http://dx.doi.org/10.5604/01.3001.0010.7718.

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Intense search for new antimicrobials, including anti-tuberculosis drugs, is dictated by the phenomenon of bacterial multidrug resistance. Hydrazides are considered the key intermediate and valuable starting material for some novel biologically active compounds. Over 70% of recently reported synthetic hydrazide derivatives are evaluated for antimicrobial and/or antifungal activity. The most frequently applied hydrazide is an anti- tuberculosis drug isoniazid/isonicotinic acid hydrazide (NIH). Hydrazide chemicals are sharing a common functional group characterized by a nitrogen- to-nitrogen covalent bond with four substituents with at least one of them being an acyl group, whereas the related hydrazines do not carry an acyl group. Hydrazides can be further classified by atom attached to the oxygen: carbohydrazides, sulfonohydrazides, phosphonic dihydrazides, hydrazone-hydrazides and phthalhydrazides. In addition to their antibacterial and antifungal activities, hydrazide derivatives have recently attracted continuing interest because of their anti-inflammatory properties. A phthalhydrazide derivative tamerit/galavit has been successfully introduced for human therapies.

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29

Shakir, Raied Mustafa, Shaimaa Abed Saoud y Dhuha Faruk Hussain. "Synthesis, Antibacterial, and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives using Vilsmeier Reagent". International Journal of Drug Delivery Technology 10, n.º 03 (25 de septiembre de 2020): 487–98. http://dx.doi.org/10.25258/ijddt.10.3.32.

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Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.

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30

Ünver, Hakan, Burak Berber, Rasime Demirel y Ayşe T. Koparal. "Design, Synthesis, Anti-Proliferative, Anti-microbial, Anti-Angiogenic Activity and In Silico Analysis of Novel Hydrazone Derivatives". Anti-Cancer Agents in Medicinal Chemistry 19, n.º 13 (11 de diciembre de 2019): 1658–69. http://dx.doi.org/10.2174/1871520619666190318125824.

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Background: Cancer is the second leading cause of death globally. Hydrazone and hydrazone derivatives have high activity, and for this reason, these compound are greatly used by researchers to synthesize new anti-cancer drug. The aim of this research work is to synthesize novel anticancer agents. Methods: New hydrazone derivatives were synthesized via a reaction between 3-formylphenyl methyl carbonate and benzhydrazide, 4-methylbenzoic hydrazide, 4-tert-butylbenzoic hydrazide, 4-nitrobenzoic hydrazide and 3- methoxybenzoic hydrazide, and were successfully characterized using elemental analysis, 1H-NMR, 13C-NMR, FT-IR and LC-MS techniques. The synthesized compounds were evaluated for their antimicrobial (some grampositive and -negative bacteria, filamentous fungi and yeasts), anti-proliferative (T47D and HCC1428-breast cancer cells) and anti-angiogenic (HUVEC-endothelial cells) activities. The anti-proliferative activities of the hydrazone compounds R1-R5 were studied on these cell lines by MTT assay. The anti-angiogenic potential of the compounds was determined by the endothelial tube formation assay. To identify structural features related to the anti-proliferative activity of these compounds, 2D-QSAR was performed. Results: The results indicated that compound R3 exhibited strong anti-angiogenic and anti-proliferative activity on breast cancer cell lines and healthy cell lines. Also, this compound; possessing a tertiary butyl moiety on the hydrazine, exhibited the highest inhibitory effect against all tested microorganisms; in particular, it inhibited Candida albicans at a lower concentration than ketoconazole. Among the investigated compounds, those bearing methyl, tertiary butyl (compound R2, R3) and methoxy (compound R5) moiety were found to be more successful anticandidal derivatives than standard antifungal antibiotics. The QSAR analysis suggested that the tumor specificity of the hydrazone correlated with their molecular weight, lipophilicity, molar refractivity, water solubility, DipolHybrid:(MOPAC) and ExchangeEnergy:(MOPAC). Absorption, Distribution, Metabolism and Elimination (ADME) analysis of the hydrazone compounds showed that they have favorable pharmacokinetic and drug-likeness properties. The ADME results clarify that R3 is the best compound in terms of pharmacokinetic properties. In contrast to other compounds; target prediction analysis of the compound R3 showed inhibitory activity on estrogen-related receptor alpha transcription factor (ESRRA). The target prediction analysis was supported by molinspiration bioactivity score. Conclusion: The R3 compound is considered to be an important candidate for future studies with its suitability for the Lipinski’s rule of five for drug-likeness, and effective in vitro and in silico results.

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31

Dammene Debbih, Ouafa, Assia Sid, Rafika Bouchene, Sofiane Bouacida, Wissam Mazouz y Noureddine Gherraf. "Two hydrazones derived from 1-aryl-3-(p-substituted phenyl)prop-2-en-1-one: synthesis, crystal structure, Hirshfeld surface analysis andin vitrobiological properties". Acta Crystallographica Section C Structural Chemistry 74, n.º 6 (22 de mayo de 2018): 703–14. http://dx.doi.org/10.1107/s2053229618006812.

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Two chalcones were synthesized by the aldolic condensation of enolizable aromatic ketones with substituted benzaldehydes under Claisen–Schmidt reaction conditions and then treated with 2,4-dinitrophenylhydrazine to yield their corresponding hydrazones. The two (E,Z)-2,4-dinitrophenylhydrazone structures, namely (Z)-1-(2,4-dinitrophenyl)-2-[(E)-3-(4-methylphenyl)-1-phenylallylidene]hydrazine, C22H18N4O4, (H1), and (Z)-1-[(E)-3-(4-chlorophenyl)-1-(naphthalen-1-yl)allylidene]-2-(2,4-dinitrophenyl)hydrazine, C25H17ClN4O4, (H2), were isolated by recrystallization and characterized by FT–IR, UV–Vis, single-crystal and powder X-ray diffraction methods. The UV–Vis spectra of the hydrazones have been studied in two organic solvents of different polarity. It was found that (H2) has a molar extinction coefficient larger than 40000. Single-crystal X-ray diffraction analysis reveals that the molecular zigzag chains of (H1) and (H2) are interconnected through noncovalent contacts. A quantitative analysis of the intermolecular interactions in the crystal structures has been performed using Hirshfeld surface analysis. All the synthesized chalcones and hydrazones were evaluated for their antibacterial and antioxidant activities. Results indicate that the studied compounds show significant activity against Gram negativeEscherichia colistrain and the chalcone 3-(4-methylphenyl)-1-phenylprop-2-en-1-one, (C1), was the most effective. In addition, only hydrazone (H1) displayed a moderate DPPH (2,2-diphenyl-1-picryl hydrazyl) scavenging efficiency.

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32

Pogonin, Aleksandr E., George A. Gamov, Maksim N. Zavalishin y Valentin A. Sharnin. "CONFORMATIONAL BEHAVIOR OF HYDRAZONE DERIVED FROM PYRIDOXAL 5’-PHOSPHATE AND ISONIAZID". IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENIY KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 61, n.º 12 (12 de diciembre de 2018): 101–7. http://dx.doi.org/10.6060/ivkkt.20186112.5846.

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The hydrazones derived from pyridoxal or pyridoxal 5’-phosphate and heterocyclic hydrazides are of interest due to their potential biological activity and metal sensing properties. These characteristics of hydrazones could be dependent on the conformation equilibria of molecule since the most stable conformer could differ from the one with the highest affinity towards biomolecule or metal ion. In the present contribution, deprotonated hydrazone formed by pyridoxal 5’-phosphate and isoniazid (PLP-INH3-) was studied by means of quantum chemistry. Three rotations leading to eight conformers are possible for this hydrazone; however, four of those species obtained by rotation of pyridine ring of isoniazid residue are degenerated. The geometry of different non-degenerated rotation conformers of the hydrazine (differing by the mutual arrangement of carbonyl group of the isoniazid residue and oxygen in 3’-site of PLP moiety) was optimized using density functional theory (B3LYP/6-311++G(d,p)). Activation barriers were evaluated. Changes in energy and geometry of conformers as well as transition states are discussed. Quantitative QTAIM (Quantum Theory of Atoms in Molecules) analysis was performed in order to check the intermolecular hydrogen bonding existence. The species capable of forming the complex with the metal ions differs from the most stable (according to the total energy values) conformer. The preliminary prediction of biological activity of PLP-INH3- hydrazone and the docking for the hydrazone and G-protein-coupled receptor kinase were performed and the preferable conformation for ligand binding to the kinase active site was found.

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33

Hishmat, O. H., S. S. Mabrouk, A. M. M. Nasef, N. M. A. Shayeb y S. A. Ismail. "Derivatives of Khellinonequinone and their Aflatoxigenic Activity". Zeitschrift für Naturforschung B 43, n.º 3 (1 de marzo de 1988): 343–46. http://dx.doi.org/10.1515/znb-1988-0318.

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Nitration of khellinone leads to the formation of a small amount of 3-nitrokhellinone and 5-acetyl-6-hydroxybenzofuran-4.7-dione (khellinonequinone) as a main product. The latter compound reacts with primary amines to give the corresponding imino compounds. Reaction of khellinone with o-phenylenediamine involves condensation followed by cyclisation. While on the other hand treating with phenyl hydrazines gives the phenyl hydrazone. The pyrazolobenzofuran derivative was obtained by the action of hydrazine hydrate on khellinonequinone. Finally the reaction with malononitrile leads to the formation of the ylidene derivative. Two quinone derivatives showed a weak effect on mycelial growth and aflatoxin formation.

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34

Tzankova, Diana, Hristina Kuteva, Emilio Mateev, Denitsa Stefanova, Alime Dzhemadan, Yordan Yordanov, Alexandrina Mateeva et al. "Synthesis, DFT Study, and In Vitro Evaluation of Antioxidant Properties and Cytotoxic and Cytoprotective Effects of New Hydrazones on SH-SY5Y Neuroblastoma Cell Lines". Pharmaceuticals 16, n.º 9 (23 de agosto de 2023): 1198. http://dx.doi.org/10.3390/ph16091198.

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A series of ten new hydrazide–hydrazone derivatives bearing a pyrrole ring were synthesized and structurally elucidated through appropriate spectral characteristics. The target hydrazones were assessed for radical scavenging activity through 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) tests, with ethyl 5-(4-bromophenyl)-1-(2-(2-(4-hydroxy-3,5-dimethoxybenzylidene)hydrazine-yl)-2-oxoethyl)-2-methyl-1H-pyrrole-3-carboxylate (7d) and ethyl 5-(4-bromophenyl)-1-(3-(2-(4-hydroxy-3,5-dimethoxybenzylidene) hydra zine-yl)-3-oxopropyl)-2-methyl-1H-pyrrole-3-carboxylate (8d) highlighted as the best radical scavengers from the series. Additional density functional theory (DFT) studies have indicated that the best radical scavenging ligands in the newly synthesized molecules are stable, do not decompose into elements, are less polarizable, and with a hard nature. The energy of the highest occupied molecular orbital (HOMO) revealed that both compounds possess good electron donation capacities. Overall, 7d and 8d can readily scavenge free radicals in biological systems via the donation of hydrogen atoms and single electron transfer. The performed in vitro assessment of the compound’s protective activity on the H2O2-induced oxidative stress model on human neuroblastoma cell line SH-SY5Y determined 7d as the most perspective representative with the lowest cellular toxicity and the highest protection.

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35

Hamed, Atef A., Hesham F. Bader y El-Sayed H. El-Ashry. "4′, x-Seco And 4′,x-4′,5′-Diseco C-Nucleosides From 2-Hydrazino-(3H)- Thieno [2,3-D] Pyrimidin-4-Ones". Zeitschrift für Naturforschung B 56, n.º 8 (1 de agosto de 2001): 826–36. http://dx.doi.org/10.1515/znb-2001-0817.

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Cyclization of 2-hydrazino-5,6-dimethyl-3H-thieno[2,3-d]pyrimidin-4-one (1) with acetic acid gave 3,6,7-trimethyl-l,2,4-triazolo[3,4-a]thieno[2,3-d] pyrimidin-5-one (5) whose Dimroth rearrangement gave 2,6,7-trimethyl-l,2,4-triazolo[3,4-a]thieno[2,3-d]pyrimidin-5-one (11). Alternatively, 5 was obtained from the dehydrogenative cyclization of acetaldehyde 5,6- dimethyl-4-3H-oxo-thieno[2,3-d]pyrimidin-2-yl hydrazone (7). Reaction of 1 and 2 with a number of sugars gave the respective hydrazones 19 and 20. Those of the D-glucose exist in the cyclic pyranosyl structure in addition to minor amounts of the acyclic structure. Dehydrogenative cyclization of the sugar hydrazones gave the respective fused tricyclic compounds 25 and 26

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36

Chandrasekhar, Vadapalli, Venkatasubbaiah Krishnan, Arunachalampillai Athimoolam y Gurusamy Thangavelu Senthil Andavan. "New hybrid inorganic-organic polymers containing cyclophosphazenes as pendant groups: Cyclophosphazene ligands containing hydrazone linkages and their conversion to polymers". Canadian Journal of Chemistry 80, n.º 11 (1 de noviembre de 2002): 1415–20. http://dx.doi.org/10.1139/v02-099.

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The reaction of the cyclotriphosphazene N3P3Cl5[O-C6H4-p-C6H4-p-CH=CH2] (2) with 10 equiv of N-methylhydrazine proceeds in a regio-specific manner to afford the multi-functional hydrazide N3P3[N(Me)NH2]5[O- C6H4-p-C6H4-p-CH=CH2] (3). Condensation of 3 with o-hydroxy benzaldehyde or pyridine-2-carboxaldehyde affords the corresponding hydrazones N3P3[N(Me)N=CH-C6H4-o-OH]5[O-C6H4-p-C6H4-p-CH=CH2] (4) and N3P3[N(Me)N=CH-C6H4N]5[O-C6H4-p-C6H4-p-CH=CH2] (5), respectively. These hydrazones can be homopolymerized to afford polymers 6 and 7 containing multi-site coordinating cyclophosphazenes as pendant groups.Key words: cyclophosphazene, hydrazone, pendant polymers, hybrid polymers, polymeric ligands.

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37

Hamada, Nagwa M. M., Sohila H. Mancy y Mohamed A. El Sekily. "A Facile Synthesis, Spectroscopic Identification, and Antimicrobial Activities of Some New Heterocyclic Derivatives from D-erythro-2,3-hexodiuloso-1,4-lactone-2-(o-chlorophenyl hydrazone)-3-oxime". International Journal of Chemistry 16, n.º 2 (4 de julio de 2024): 62. http://dx.doi.org/10.5539/ijc.v16n2p62.

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A new series of different heterocyclic derivatives was prepared via a facile unimolecular condensation of D-iso ascorbic acid with o-chlorophenyl hydrazine to give D-erythro-2,3-hexodiulosono-1,4-lactone 2-( o-chlorophenyl hydrazine (2). Reactions of (2) with hydroxylamine gave the 2-( o-chlorophenyl hydrazone)-3-oxime (3). On boiling with boiling acetyl chloride, (3) gave 2-o-chlorophenyl-4-(2,3-di-O-acetyl-D-erythro-glyceryl-1-yl)-1,2,3-triazole-5-carboxylic acid-5,1́-lactone (4). In the treatment of (3) with benzoyl chloride in pyridine the same dehydrative cyclization occurred giving, 2-o-chlorophenyl-4-(2,3-di-o-benzoyloxy-D-erythro-glycerol-1-yl)-1,2,3-triazole-5-carboxylic acid-5,1΄-lactone (5). On the treatment of compound (4) with liquid ammonia in methanol, deacetylation occurred concurrently with the opening of the lactone ring, to afford the 2-o-chlorophenyl-4-(D-erythro-glycerol-1-yl)-1,2,3-triazole-5-carboxamide (6). Similarly, treatment of compound (4) with hydrazine hydrate in methanol, afforded 2-o-chlorophenyl-4-(D-erythro-glycerol-1-yl)-1,2,3-triazole-5-carboxylic acid hydrazide (7).  The controlled reaction of (3) with sodium hydroxide, followed by neutralization, gave 3-(D-erythro-glycerol-1-yl)-4,5-isoxazoline-5-(4H)-one-4-o-chlorophenyl hydrazone (8). Reaction of (3) with HBr-AcOH gave 5-O-acetyl-6-bromo-6-deoxy-D-erythro-2,3-hexodiulosono-1,4-lactone-2-(o-chlorophenyl hydrazone)-3-oxime (9); these were converted into 4-(2-O-acetyl-3-bromo-3-deoxy-l-threo-glycerol-l-yl)-2-aryl-1,2,3-triazole-5-carboxylic acid 5,41-lactones on treatment with acetic anhydride-pyridine. Compound (3) treatment with bromine-water caused its cyclization and bromination of the phenyl group to give carboxylic acid 5,1΄-lactone (10). Acetylation of (10) gave the diacetate (11), which upon treatment with hydrazine hydrate in methanol, afforded compound (12), mild acetylation of compound (12) gave the triacetate (13) boiling of (13) with acetic anhydride afforded hexa acetyl derivative (14). on the treatment of compound (11) with liquid ammonia in methanol deacetylation occurred to afford 1,2,3-triazole-5-carboxamide derivative (15). On the other hand, treatment of compound (3) with bromine-water for a short time yielded 3-oxime (16). Subsequent acetylation with boiling acetic anhydride afforded compound (11). In addition, acetylation of compound 3 afforded a diacetyl derivative assigned as 5,6-di-O-acetyl-D-erythro-2,3-hexodilusono-1,4-lactone-(2-o-chlorophenyl hydrazone)-3-acetoxime (17), which on boiling with acetic anhydride cyclization occurred giving compound (4). On the treatment of Dehydro-L-ascorbic acid-2-phenyl hydrazone (L-threo-2,3-hexodiulosono- 1,4-lactone 2-phenylhydrazone (19) with acetic anhydride/pyridine, afforded 5,6-di-O-acetyl-3-acetoxime (20) that upon treatment with boiling acetic anhydride, afforded the triazole derivative (21). Furthermore, treatment of the monophenyl hydrazone (18) with S-benzyl hydrazine carbodithiolate in the presence of acetic acid, afforded the bis-hydrazone, L-threo-2,3-hexodilusono-1,4-lactone-3-(S-benzylhydrazinocarbodithiolate)-2-phenylhydrazone (22). Acetylation of compound (22) with acetic anhydride and pyridine did not give the di-O-acetyl derivative expected but instead, elimination of a molecule of acetic acid and partial hydrolysis of a hydrazone residue took place to give compound (23). The structures of all the synthesized compounds were confirmed using elemental analysis and different spectral tools. Eight samples from the synthesized compounds, 2,3, 4,10.16,11,12,17 were tested for their antimicrobial activity and they showed no activities.

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Journal, Baghdad Science. "Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid". Baghdad Science Journal 7, n.º 1 (7 de marzo de 2010): 727–36. http://dx.doi.org/10.21123/bsj.7.1.727-736.

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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid chloride derivative(4), followed by conversion into the corresponding acid hydrazide derivative (5) carboxylic acid thiosemicarbazide (11), esters (14,15), thioesters (16,17) and amides (18,19), when treated hydrazine hydrate, thiosemicarbazide, alcohols, alkylthiol and secondary amines in dry refluxing benzene; respectively. Schiff's bases (6-8) were prepared by refluxing of compound (5) with different aldehydes and ketons, then two compounds from the Schiff's bases were cyclized with ?-mercapto acetic acid to give (9 and 10). Furthermore, 1,2,4-triazole derivative (12) have been also prepared by refluxing thiosemicarbazide derivative with sodium hydroxide solution (4%) followed acidification of the result using (10%)hydrolic acid. Moreover, a thiadiazole derivative (13) has been prepared by treatment of thiosemicarbazide derivative with concentrated sulfuric acid as cyclyzing agent. Finally, oxadiazole derivative (20) has prepared by condensation of its acid hydrazide derivative with carbon disulfide in basic medium.

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Ananthi, Vadamalai, Kaliyaraj Rajalakshmi, Inbasekaran Muthuvel y Ganesamoorthy Thirunarayanan. "Solid acidic FeCl3/Bentonite catalyzed solvent-free condensation: Synthesis, spectral studies and antimicrobial activities of some aryl hydrazine Schiff’s bases". Annales Universitatis Mariae Curie-Sklodowska, sectio AA – Chemia 71, n.º 2 (3 de abril de 2017): 127. http://dx.doi.org/10.17951/aa.2016.71.2.127.

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Some aryl hydrazide derivatives have been synthesized including 1-(3-chloro-4-nitrophenyl)-2-(3-substituted benzylidene) hydrazines by FeCl3/Bentonite catalyzed solvent-free condensation of substituted phenyl hydrazine and aldehydes under microwave irradiation. The yields of the hydrazides are more than 70%. The synthesized hydrazides are characterized by the physical constants, micro analysis and spectroscopic data. Effect of catalyst, solvent effect substituent effect and optimization of the catalyst was studied by the percentage of isolated yields. From the catalyst optimization, the present study catalyst gave the better yield of products. The antimicrobial activities of all synthesized of 1-(3-chloro-4-nitrophenyl)-2-(3-substituted benzylidene) hydrazines have been evaluated using Bauer-Kirby disc diffusion method.

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40

Fatullayeva, P. A. "COMPLEXES OF METALS WITH HYDRAZONE HYDRAZIDE SALICYLIC ACID". Chemical Problems 19, n.º 2 (2021): 79–83. http://dx.doi.org/10.32737/2221-8688-2021-2-79-83.

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Complexes of Cu (II), Ni (II), and Co (II) with hydrazone derivatives of salicylic acid hydrazide and 3,5-di-tert-butyl salicylic aldehyde (LH) were synthesized and the structure of these compounds studied by means of elemental analysis methods, IR and electronic spectroscopy, magnetochemistry and thermal analysis. It revealed that the complexes are monomeric and have a composition [MLXSoI] where M is a metal ion, L is a ligand, X is an inorganic anion, and Sol is a solvent molecule. LH- in the complexes behaves like a monoanionic tridentate ligand. It found that the resulting complexes exhibit noticeable inhibitory and urease activity.

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Jasril, E. Juwiyatri, S. N. Fauza y N. Afriana. "Synthesis, in vitro Antioxidant Activity, and Toxicity Evaluation of Hydrazone Derivatives Naphthalene-1-ylmethylene hydrazine". Journal of Physics: Conference Series 2049, n.º 1 (1 de octubre de 2021): 012050. http://dx.doi.org/10.1088/1742-6596/2049/1/012050.

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Abstract Hydrazone is a versatile organic compound that has a basic structure (-NHN=CH-) called the azomethine group. This structure is responsible for the physical and chemical of hydrazone, which makes this compound has variety bioactivities such as antioxidant, antitumor, and anticancer. In this work, two hydrazone derivatives from 1-naphthaldehyde and hydrazine (phenylhydrazine/hydrazine hydrate) have been synthesized under microwave irradiation. Their antioxidant activity and toxicity were evaluated by DPPH and BSLT method, respectively. Structures of the synthesized compounds were confirmed based on spectroscopic data included UV, FTIR, HRMS, and 1H-NMR. Based on the DPPH assay, hydrazone from phenylhydrazine has strong antioxidant (IC50 28.90 μg/mL) but inactive antioxidant for hydrazine hydrate (IC50 >1000 μg/mL). However, both compounds have a high toxicity effect on Artemia Salina Leach with each LC50 1.45 and 47.20 μg/mL, hence they have the potential to be developed into anticancer drugs.

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42

Refat, Moamen S., Ahmed Gaber, Walaa F. Alsanie, Mohamed I. Kobeasy, Rozan Zakaria y Kehkashan Alam. "Utilization and simulation of innovative new binuclear Co(ii), Ni(ii), Cu(ii), and Zn(ii) diimine Schiff base complexes in sterilization and coronavirus resistance (Covid-19)". Open Chemistry 19, n.º 1 (1 de enero de 2021): 772–84. http://dx.doi.org/10.1515/chem-2021-0068.

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Abstract This article aimed at the synthesis and molecular docking assessment of new diimine Schiff base ligand, namely 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxyvinyl)hydrazono) methyl)-6-methoxyphenol (methoxy-diim), via the condensation of 1-(4-chloro-phenyl)-2-hydrazino-ethenol compound with 2-((E)-(2-((Z)-2-(4-chlorophenyl)-2-hydroxy vinyl) hydrazono)methyl)-6-methoxyphenol in acetic acid as well as the preparation of new binuclear complexes of Co(ii), Ni(ii), Cu(ii), and Zn(ii). The following synthesized complexes were prepared in a ratio of 2:1 (metal/ligand). The 1H-NMR, UV-Vis, and FTIR spectroscopic data; molar conductivity measurements; and microanalytical, XRD, TGA/DTG, and biological studies were carried out to determine the molecular structure of these complexes. According to the spectroscopic analysis, the two central metal ions were coordinated with the diamine ligand via the nitrogen of the hydrazine and oxygen of the hydroxyl groups for the first metal ions and via the nitrogen of the hydrazine and oxygen of the phenol group for the second metal ions. Molecular docking for the free ligand was carried out against the breast cancer 3hb5-oxidoreductase and the 4o1v-protein binding kidney cancer and COVID-19 protease, and good results were obtained.

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Kalaiarasi, N. y S. Manivarman. "Spectral characterization, microbial activities and toxicity study of some newly synthesized hydrazone derivatives". International Journal of Advanced Chemistry 5, n.º 2 (22 de junio de 2017): 54. http://dx.doi.org/10.14419/ijac.v5i2.7739.

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Hydrazone derivatives of 2-Thioxodihyropyrimidine-2-dione were synthesized by addition of thiobarbituric acid with phenyl hydrazine, dinitrophenyl hydrazine, semicarbazide, thiosemicarbazide and benzohydrazide respectively. Structures of these synthesized compounds are characterized by means of UV, IR, Proton-NMR, Carbon- NMR. Finally the hydrazone derivatives synthesized are screened for biological activities namely antibacterial and antifungal activities. Also in addition the toxicity studies of the compounds are also performed.

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Al-Humaidi, Jehan Y., Mohamed G. Badrey, Ashraf A. Aly, AbdElAziz A. Nayl, Mohie E. M. Zayed, Ohoud A. Jefri y Sobhi M. Gomha. "Evaluation of the Binding Relationship of the RdRp Enzyme to Novel Thiazole/Acid Hydrazone Hybrids Obtainable through Green Synthetic Procedure". Polymers 14, n.º 15 (3 de agosto de 2022): 3160. http://dx.doi.org/10.3390/polym14153160.

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The viral RNA-dependent RNA polymerase (RdRp) complex is used by SARS-CoV-2 for genome replication and transcription, making RdRp an interesting target for developing the antiviral treatment. Hence the current work is concerned with the green synthesis, characterization and docking study with the RdRp enzyme of the series of novel and diverse hydrazones and pyrazoles. 4-Methyl-2-(2-(1-phenylethylidene)hydrazineyl)thiazole-5-carbohydrazide was prepared and then condensed with different carbonyl compounds (aldehydes and ketones either carbocyclic aromatic or heterocyclic) afforded the corresponding hydrazide-hydrazones. The combination of the acid hydrazide with bifunctional reagents such as acetylacetone, β-ketoesters (ethyl acetoacetate and ethyl benzoylacetate) resulted in the formation of pyrazole derivatives. The synthesized compounds were all obtained through grinding method using drops of AcOH. Various analytical and spectral analyses were used to determine the structures of the prepared compounds. Molecular Operating Environment (MOE®) version 2014.09 was used to estimate interactions between the prepared thiazole/hydrazone hybrids and RdRp obtained from the protein data bank (PDB: 7bv2) using enzyme-ligand docking for all synthesized derivatives and Remdesivir as a reference. Docking results with the RdRp enzyme revealed that the majority of the investigated drugs bind well to the enzyme via various types of interactions in comparison with the reference drug.

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Abo-Ghalia, Mohamed H., Abd El-Galil E. Amr y Mohamed M. Abdalah. "Synthesis of Some New (Nα-Dipicolinoyl)-bis-L-leucyl-DL-norvalyl Linear tetra and Cyclic octa Bridged Peptides as New Antiinflammatory Agents". Zeitschrift für Naturforschung B 58, n.º 9 (1 de septiembre de 2003): 903–10. http://dx.doi.org/10.1515/znb-2003-0912.

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In continuation to our search for new amino acid and peptide based anti-inflammatory agents, the suggestion, synthesis, structure elucidation of some Nα -bis-dipicolinoyl amino acids, linear tetra and cyclic octa bridged peptides 1-9, of which four are new compounds 6-9, were herein realized. Accordingly, Nα -bis-dipicolinoyl-L-leucine methyl ester 1, the corresponding acid 2, its bis-DL-norvalyl methyl ester homologue 3, the acid 4 and hydrazide 5 analogues were conventionally prepared.The tetrachlorophthalic acid hydrazine conjugate 6, anisaldehyde hydrazone 7, the benzenetetracarboxylic acid and naphthalenetetracarboxylic acid bis-L-leucyl-DL-norvalyl cyclic octa bridged peptides 8 and 9 respectively, were newly synthesized via condensation of the hydrazide 5 with the corresponding aldehyde or anhydride.The chromatographic, IR, NMR and mass spectral analysis confirmed the identities of the synthesized compounds.Comparable to the two reference antiinflammatory drugs indomethacin® and voltaren® (100%), the determined antiinflammatory potency of the candidates (carrageenan® induced paw edema in rats) revealed a general significant activity (66 - 94%), except for the practically inactive 6 (∼1.5 % activity).In particular, the potency of the (Nα -dipicolinoyl)-bis-L-leucyl-DL-norvalyl anisaldehyde hydrazone 7 was of 94 and 87%, comparable to the reference drugs. However, 7 also showed 58% protection against ulcer formation, comparable to null for indomethacin®. Additionally, an acceptable acute toxicity was observed (LD50: 2833 mg/kg, comparable to 2700 and 2850 for indomethacin® and voltaren® respectively).

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Abood, Huda Saleh, Ekhlas Qanber Jasim y Munther Abduljaleel Muhammad-Ali. "Synthesis, Corrosion Inhibition Efficiency in Acidic Media, and Quantum Chemical Studies of Some Hydrazine Derivatives". Science and Technology Indonesia 9, n.º 1 (22 de enero de 2024): 137–47. http://dx.doi.org/10.26554/sti.2024.9.1.137-147.

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In this work, four hydrazone Schiff base derivatives N-(2,4-Dinitro-phenyl)-N’-(1H-pyrrol-2-ylmethylene)-hydrazine (1a), N-Benzo [1,3] dioxol-5-ylmethylene-N’-(2,4-dinitro-phenyl)-hydrazine (1b), (E)-5-((2-(2,4-dinitrophenyl)hydrazono)methyl)-2-hydroxybenzoic acid (1c) and (E)-1-(2,4-dinitrophenyl)-2-(2-methoxybenzylidene)hydrazine (1d) were synthesized by reaction of four aldehydes namely pyrrole-2-carboxaldehyde, piperonal, 5-formylsalicylic acid, and o-vanillin with 2,4-dinitrophenyl hydrazine to produce the final compounds 1a, 1b, 1c, and 1d, respectively. These four compounds were investigated as corrosion inhibitors in aqueous mild acidic static solution. FTIR, HNMR, and elemental analysis were used to elucidate the chemical structure of the synthesized inhibitors. Using potential dynamic polarization measurements, these inhibitors’ efficiency in preventing C-steel corrosion in 1.00 M HCl was studied. The results of the experiments revealed that 1×10−3 M is the ideal concentration for 1a, 1b, 1c, and 1d, and that the corresponding inhibition efficiencies for these subunits were 80.70%, 91.30%, 91.34, and 88.80%, respectively. The best corrosion inhibitors were compounds 1b and 1c. Furthermore, studies suggested that these substances are mixed-type inhibitors and that the efficiency of the inhibition is strongly correlated with their quantity. Quantum paraments included Dipole moment, energy band gap (ΔE), value of energy of lowermost unoccupied molecular orbital (ELUMO), and energy of high most occupied molecular orbital (EHOMO) using Molecular Operating Environment MOE, Gaussian, and HyperChem software packages were determined which demonstrated strong agreement between algorithmic and practical findings.

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M. Samir, E. y R. M. Mohareb. "Novel synthesis of pyran-3-hydrazide derivatives and their uses to the synthesis hydrazide-hydrazone, pyrazole and thiazole derivatives with anticancer activities". Bulletin of the Chemical Society of Ethiopia 35, n.º 3 (31 de enero de 2022): 573–86. http://dx.doi.org/10.4314/bcse.v35i3.9.

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ABSTRACT. The multi-component reaction of ethyl acetoacetate with each of malononitrile (3) benzaldehyde (1) in ethanol containing triethylamine gave the ethyl 6-amino-5-cyano-2-methyl-4-phenyl-4H-pyran-3-carboxylate (4). The latter compound reacted with hydrazine hydrate to give the hydrazide derivative 6. Compound 6 underwent a series of hetero-cyclization reactions to give pyrzole, hydraide-hydrazone, thiazole derivatives. The produced compounds tested against cancer cell lines six cancer cell lines and showed that compounds 8b, 10b, 11a, 17a, 21 and 24a were the most cytotoxic compounds. Further tests of the latter compounds toward the five tyrosine kinases and Pim-1 kinase showed that compounds 10b, 21 and 24a were the most potent of the tested compounds and compounds 10a, 11a and 17a were of the highest inhibitions toward Pim-1 kinase. The high inhibitions of most of the tested compounds toward the selected cancer cell lines and the tyrosine kinases encourage for future work to be done. KEY WORDS: Hydrazide, Thiophene, Pyrazole, Pyran, Cytotoxicity, Tyrosine kinases Bull. Chem. Soc. Ethiop. 2021, 35(3), 573-586. DOI: https://dx.doi.org/10.4314/bcse.v35i3.9

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KushalNath Mishra, Shambaditya Goswami, Kumudhavalli M.V, Kamal Saini, Nikita Pal, Nilesh Sharma y Pragya Pandey. "Hydrazones and their metal complexes: A short review on their biological potentia". International Journal of Research in Pharmaceutical Sciences 11, SPL4 (21 de diciembre de 2020): 1440–47. http://dx.doi.org/10.26452/ijrps.v11ispl4.4319.

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Hydrazones belong to complexes are beneficial in different fields for their essential role in the development of a range of stable complexes in the coordination chemistry. Different researchers have reported the various medicinal properties of hydrazones. Hydrazone and its metal complexes are useful for the detection of some organic components from pharmaceutical formulations. These metallic compounds act as a catalyst for conducting various chemical reactions and help in making different chemical complexes that are effective against bacteria, fungi, and many other microbes. Aromatic hydrazone derivatives can measure the concentration of low molecular weight aldehyde and ketone complexes. Hydrazones possess numerous medicinal properties, including antimicrobial, anti-cancer, antidepressant, anti-tubercular, anti-viral, etc. For the new drug discovery, hydrazones/azomethines are considered to be an important class of compound. From molecular biology to pharmaceutical formulation, organic chemistry, new drug development process, the importance of hydrazone and its metal complexes is immense. The present review aims to highlight the reported biological activities related to hydrazones for the last decade.

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Ristić, Milenko, Biljana Dekić, Niko Radulović y Marija Aksić. "Synthesis, complete assignment of 1H- and 13C-NMR spectra and antioxidant activity of new azine derivative bearing coumarin moiety". Bulletin of Natural Sciences Research 11, n.º 1 (2021): 9–16. http://dx.doi.org/10.5937/bnsr11-31265.

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In this research, the synthesis of a new azine derivative with coumarin moiety was performed in three reaction steps, starting from 4-hydroxycoumarin. The first step in synthesis was the acetylation of 4-hydroxycoumarin to yield 3-acetyl-4-hydroxycoumarin and then the obtained 3-acetyl-4-hydroxycoumarin was reacted with hydrazine hydrate and give a corresponding hydrazone. Condensation of the hydrazone with 4-ethoxy-3methoxybenzaldehyde afforded the target compound 1-[1-(4-hydroxy-2-oxo-2H-chromen-3-yl)-ethylidene]-2-(4etoxy-3-methoxybenzylidene)-hydrazine in a good yield. The resulting azine derivative is fully spectrally characterized, including complete assignment of 1Hand 13C-NMR spectra, as well as 2D NMR (1H1H COSY, NOESY, HSQC and HMBC) spectra. The antioxidant activity of corresponding hydrazone and target compound was evaluated by DPPH method where hydrazone derivative displayed a significant and target azine good antioxidant activity, with IC50 (mM) values 11.69 and 216.60, respectively.

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Suleman, Veyan Taher y Abdul Ghany Mohammed Al-Daher. "Synthesis, Characterization, Density Functional Theory Studies and Antioxidant Activity of Novel Hydrazone Ligands and their Metal Complexes". Oriental Journal Of Chemistry 39, n.º 6 (27 de diciembre de 2023): 1629–42. http://dx.doi.org/10.13005/ojc/390624.

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Novel hydrazone ligands (HL) derived from 2,5-hexandione and benzoyl hydrazine (HDBH), 2-furoyl hydrazine (HDFH), or 2-picolinoyl hydrazine (HDPH) were used to synthesize mononuclear Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) complexes of the general formula [M(L)2].xH2O (x= 0-3). The hydrazone ligands and the isolated complexes were characterized by, spectral, thermal analysis, molar conductance, and magnetic moment measurements. Beside, density functional theory (DFT) computations have been to study structures and energetic of the ligand and its complexes. The IR spectral information suggests that the ligands exhibit monobasic tridentate behavior through their ONO donor atoms. The metal complexes were determined to possess monomeric octahedral geometry. The DPPH antioxidant capability of both the ligand and their metal complexes was evaluated.

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