Статті в журналах: "Thio semicarbazides"

1

Chen, Wen-Bin, and Gui-Yu Jin. "Synthesis ofn-(thio)phosphoryl-n?-2-benzoxazolyl semicarbazides." Heteroatom Chemistry 12, no. 3 (2001): 151–55. http://dx.doi.org/10.1002/hc.1024.

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2

Hemdan, Magdy M. "Addition–cyclisation of 3-(2-thienyl)acryloyl isothiocyanate with hydrazine derivatives as a source of triazoles and thiadiazoles." Journal of Chemical Research 2009, no. 8 (August 2009): 489–91. http://dx.doi.org/10.3184/030823409x12474221035136.

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3-(2-Thienyl)acryloyl isothiocyanate reacts additively with hydrazine hydrate, phenylhydrazine, 2-pyridyl hydrazine, (thio) semicarbazides, as well as benzoyl- and ethoxycarbonyl hydrazine. Simultaneous or subsequent cyclisation of the resulting 1:1 adducts in acidic or alkaline media yields substituted 1,3,4-thiadiazoles or 1,2,4-triazoles respectively.

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3

Chen, Wen-Bin, and Gui-Yu Jin. "ChemInform Abstract: Synthesis of N-(Thio)phosphoryl-N′-2-benzoxazolyl Semicarbazides." ChemInform 32, no. 32 (May 25, 2010): no. http://dx.doi.org/10.1002/chin.200132175.

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4

Yogeeswari, P., D. Sriram, V. Saraswat, J. Vaigunda Ragavendran, M. Mohan Kumar, S. Murugesan, R. Thirumurugan, and J. P. Stables. "Synthesis and anticonvulsant and neurotoxicity evaluation of N4-phthalimido phenyl (thio) semicarbazides." European Journal of Pharmaceutical Sciences 20, no. 3 (November 2003): 341–46. http://dx.doi.org/10.1016/j.ejps.2003.08.002.

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5

Wujec, Monika, Ewa Kędzierska, Edyta Kuśmierz, Tomasz Plech, Andrzej Wróbel, Agata Paneth, Jolanta Orzelska, Sylwia Fidecka, and Piotr Paneth. "Pharmacological and Structure-Activity Relationship Evaluation of 4-aryl-1-Diphenylacetyl(thio)semicarbazides." Molecules 19, no. 4 (April 16, 2014): 4745–59. http://dx.doi.org/10.3390/molecules19044745.

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6

Alshammari, Mohammed B., Ashraf A. Aly, Stefan Bräse, Martin Nieger, and Lamiaa E. Abd El-Haleem. "Efficient Synthesis of Various Substituted (Thio)Ureas, Semicarbazides, Thiosemicarbazides, Thiazolidones, and Oxadiazole Derived from [2.2]Paracyclophane." ACS Omega 7, no. 15 (April 6, 2022): 12879–90. http://dx.doi.org/10.1021/acsomega.2c00141.

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7

Awad, Ibrahim M. A., Abdu E. Abdel-Rahman, and Etify A. Bakhite. "Synthesis and application of some new S-(substituted)thio- and thienoquinoline derivatives as antimicrobial agents." Collection of Czechoslovak Chemical Communications 56, no. 8 (1991): 1749–60. http://dx.doi.org/10.1135/cccc19911749.

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Ethyl (4-aryl-3-cyano-5,6,7,8-tetrahydro-2-quinolinylthio) acetate (IIa, IIb) were prepared and reacted with hydrazine hydrate to give hydrazines IIIa, IIIb which underwent cyclization into thienoquinoline derivatives IVa, IVb. Reaction of IIIa, IIIb with phenyl isocyanate yielded semicarbazides Va, Vb. Similarly, IIIa, IIIb and IVb were interacted with methyl/phenyl isothiocyanates affording the corresponding thiosemicarbazide derivatives VIa - VId and XIVa, XIVb respectively. On the other hand, condensation of IIIb with acetylacetone gave the pyrazole VII treatment with ethoxide furnished VIII. Also, IIIa, IIIb and IVa, IVb reacted with aromatic aldehydes to afford hydrazones IXa - IXf and XIa - XIf respectively. Cyclodehydration of IXd - IXf with thioglycolic acid furnished 4-thiazolidinone derivatives Xa - Xc. Moreover, IVb was reacted with formic acid/acetic anhydride to give XII and XIII. Diazotization of IVb gave azide XV which underwent Curtius rearrangement into XVI. The structures of all newly synthesized compounds were confirmed by elemental analyses and spectral data. Also, the most of these compounds were tested in vitro for their antimicrobial activities against some Gram-positive and Gram-negative bacteria.

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8

Aksenov, Nicolai A., Nikolai A. Arutiunov, Nikita K. Kirillov, Dmitrii A. Aksenov, Alexander V. Aksenov та Michael Rubin. "Preparation of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles via chemoselective сyclocondensation of electrophilically activated nitroalkanes to (thio)semicarbazides or thiohydrazides". Chemistry of Heterocyclic Compounds 56, № 8 (серпень 2020): 1067–72. http://dx.doi.org/10.1007/s10593-020-02775-5.

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9

Eldehna, Wagdy M., Hadia Almahli, Tamer M. Ibrahim, Mohamed Fares, Tarfah Al-Warhi, Frank M. Boeckler, Adnan A. Bekhit, and Hatem A. Abdel-Aziz. "Synthesis, in vitro biological evaluation and in silico studies of certain arylnicotinic acids conjugated with aryl (thio)semicarbazides as a novel class of anti-leishmanial agents." European Journal of Medicinal Chemistry 179 (October 2019): 335–46. http://dx.doi.org/10.1016/j.ejmech.2019.06.051.

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10

Fernandes, Tiago A., Vânia André, Aliaksandr S. Arol, Ângela França, Sergei Mikhalyonok, Nuno Cerca, and Alexander M. Kirillov. "New silver (thio)semicarbazide derivatives: synthesis, structural features, and antimicrobial activity." New Journal of Chemistry 44, no. 26 (2020): 10924–32. http://dx.doi.org/10.1039/d0nj02013c.

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11

Lohar, Sisir, Sougata Sinha, Subrata Ghosh, and Debasis Das. "Tri-color emission and colorimetric recognition of acetate using semicarbazide and thio-semicarbazide derivatives: Experimental and computational studies." Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 155 (February 2016): 75–80. http://dx.doi.org/10.1016/j.saa.2015.10.018.

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12

Uzbekov, Marat G. "Pathogenetic Mechanisms of Mental Disorders: Endogenous Intoxication." Biochemistry (Moscow) 88, no. 4 (April 2023): 491–501. http://dx.doi.org/10.1134/s0006297923040053.

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Abstract The review describes the syndrome of endogenous intoxication in patients with mental disorders. Oxidative stress, middle-mass endotoxic molecules, impaired functional properties of serum albumin and albumin thiol groups, neurotrophic factors, and enzymes, including monoamine oxidase and semicarbazide-sensitive amine oxidase contribute to the development of endogenous intoxication. Possible pathogenetic mechanisms of the endogenous intoxication development in mental disorders and approaches to its treatment are discussed.

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13

Malhotra, Rajesh. "Novel Bioactive Thio- and Semicarbazide Ligands and Their Organosilicon (IV) Complexes." Phosphorus, Sulfur, and Silicon and the Related Elements 185, no. 9 (August 25, 2010): 1875–85. http://dx.doi.org/10.1080/10426500903348021.

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14

Aljamali, Nagham Mahmood, Nour Abd Alrazzak Abd Allattif, and Sabreen Ali Abdalrahman. "Cyclization of Multi Components Reactions and (Preparation, Investigation, Thermal Curves)." American International Journal of Multidisciplinary Scientific Research 2, no. 1 (October 10, 2018): 1–12. http://dx.doi.org/10.46281/aijmsr.v2i1.190.

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Many cyclic compounds were formatted via multi components reactions and cyclization reaction through many steps with ( various conditions , various starting materials , various components ), in first step , aromatic amine derivative were reacted with ammonium thiocyanate in cyclization reaction to yield 2-aminobenzothiazole derivative , which reacted with formaldehyde and benzaldehyde as a multi components reaction ., then the resulting compounds cyclized with ( semicarbazide , ortho-phenyl diamine , ortho-thiol aniline , ortho- amino phenol ). Investigation of compounds carried out through many techniques ( FT.IR , H.NMR , Mass ) – Spectra , Thermal studies

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15

Allahverdiyeva, G. E., V. M. Ismailov, I. A. Mamedov, and N. N. Yusubov. "Reactions of triethyl phosphonoacetate, bromoacetaldehyde diethyl acetal, and (diethoxyphosphoryl)acetaldehyde with thiourea and (thio)semicarbazide." Журнал общей химии 93, no. 5 (May 15, 2023): 711–16. http://dx.doi.org/10.31857/s0044460x23050062.

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Condensation of thiocarbamide with triethyl phosphonoacetate leads to S -phosphorylated 2-ethoxy-4-oxo3,4,5-trihydro-1,5,2-diazaphosphinine-2-oxide, an isostere of thiobarbiturate. Under similar conditions, triethyl phosphonoacetate reacts with semicarbazide with the intermediate formation of 2-(diethoxyphosphorylacetyl) hydrazine-1-carboxamide, which forms a triazine upon cleavage of the P-C bond and 1,2,3-phosphadiazole upon cleavage of the C-N bond. Under analogous conditions, the condensation of triethyl phosphonoacetate with thiosemicarbazide proceeds with cleavage of the Р-С bond and heterocyclization with the formation of the 1,3,4-thiadiazine derivative. Upon condensation of bromoacetaldehyde diethyl acetal with thiosemicarbazide, 4 H -1,3,4-thiadiazine-2-amine was formed. (Diethoxyphosphoryl)acetaldehyde reacts with thiosemicarbazide under the same conditions in a ratio of 1:2, forming a linear product, thiophosphatoiminohydrazone of (diethoxyphosphoryl)acetaldehyde.

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16

Song, Gaopeng, Jianzuo Li, Hao Tian, Yasheng Li, Dekun Hu, Ying Li, and Zining Cui. "Synthesis and Antitumor Activity of Novel N-Benzoyl-N'-substituted Pyrimidinyl (Thio)semicarbazide Derivatives." Letters in Drug Design & Discovery 13, no. 4 (March 3, 2016): 329–34. http://dx.doi.org/10.2174/1570180812666151003002644.

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17

Liang, Zhaochang, Yuping Huang, Shiben Wang, and Xianqing Deng. "Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents." Letters in Drug Design & Discovery 16, no. 9 (September 11, 2019): 1020–30. http://dx.doi.org/10.2174/1570180816666190325163117.

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Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

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18

Allahverdiyeva, G. E., V. M. Ismailov, I. A. Mamedov, and N. N. Yusubov. "Reactions of Triethyl Phosphonoacetate, Bromoacetaldehyde Diethyl Acetal, and (Diethoxyphosphoryl)acetaldehyde with Thiourea and (Thio)semicarbazide." Russian Journal of General Chemistry 93, no. 5 (May 2023): 1064–68. http://dx.doi.org/10.1134/s1070363223050067.

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19

Li, Shaoyuan, Wenhui Ma, Xiuhua Chen, Cong Zhang, Xiao He, Yudong Shang, Yuxin Zou, and Zhengjie Chen. "Fabrication of an Innovative Lead-Ions Sensitive Electrode Based on Thio-semicarbazide Derivative Modified Nanoporous Silicon." Current Environmental Engineering 3, no. 3 (December 20, 2016): 267–72. http://dx.doi.org/10.2174/2212717803666160725152731.

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20

Jeyashri, K. R., Y. Baby, E. Dhineshkumar, M. Seenivasan, and H. Manikandan. "Synthesis, spectral and theoretical studies of some 3-benzylidene amino-1,2,3-triarylpropan-1-one thio/semicarbazide." Materials Today: Proceedings 51 (2022): 2300–2308. http://dx.doi.org/10.1016/j.matpr.2021.11.408.

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21

Hajalsiddig, Tawassl Tajelsir Hassan, and Ahmed Elsadig Mohammed Saeed. "Synthesis of new 6-substituent 2-phenyl and 2-(furan-2-yl)-3-phenyl-quinoline-4-carboxylic acid derivatives." European Journal of Chemistry 10, no. 1 (March 31, 2019): 57–63. http://dx.doi.org/10.5155/eurjchem.10.1.57-63.1816.

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A synthesis of substituted quinolines has been achieved by the Doebner reaction which is a three component coupling of arylaldehyde, p-amino-acetophenone and phenyl pyruvic acid. The products of 2,3-diary-6-acetyl-quinoline-4-carboxylic acids were obtained by Claisen Schmidt condensation reaction with aldehydes in the presence of sodium hydroxide in order to give the corresponding α,β-unsaturated carbonyls. The substituted α,β-unsaturated carbonyls were condensed with urea, thiourea, hydrazine, phenyl hydrazine, semicarbazide hydrochloride and ethanolamine to synthesized 2-pyrimidinone, 2-pyrimidinethion, pyrazoline-1-phenyl, pyrazoline, pyrazoline-1-carboxamide and 1,4-oxazepines derivatives, respectively, with good yields. The purity and identities of products were elucidated through thin layer chromatography (TLC), melting point and spectroscopic data (IR, 1H NMR, 13C NMR and LC-Mass).

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22

Tumosienė, Ingrida, Kristina Kantminienė, Arnas Klevinskas, Vilma Petrikaitė, Ilona Jonuškienė, and Vytautas Mickevičius. "Antioxidant and Anticancer Activity of Novel Derivatives of 3-[(4-Methoxyphenyl)amino]propanehydrazide." Molecules 25, no. 13 (June 29, 2020): 2980. http://dx.doi.org/10.3390/molecules25132980.

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Series of novel 3-[(4-methoxyphenyl)amino]propanehydrazide derivatives bearing semicarbazide, thiosemicarbazide, thiadiazole, triazolone, triazolethione, thiophenyltriazole, furan, thiophene, naphthalene, pyrrole, isoindoline-1,3-dione, oxindole, etc. moieties were synthesized and their molecular structures were confirmed by IR, 1H-, 13C-NMR spectroscopy and mass spectrometry data. The antioxidant activity of the synthesized compounds was screened by DPPH radical scavenging method. The antioxidant activity of N-(1,3-dioxoisoindolin-2-yl)-3-((4-methoxyphenyl)amino)propanamide and 3-((4-methoxyphenyl)amino)-N’-(1-(naphthalen-1-yl)-ethylidene)propanehydrazide has been tested to be ca. 1.4 times higher than that of a well-known antioxidant ascorbic acid. Anticancer activity was tested by MTT assay against human glioblastoma U-87 and triple-negative breast cancer MDA-MB-231 cell lines. In general, the tested compounds were more cytotoxic against U-87 than MDA-MB-231 cell line. 1-(4-Fluorophenyl)-2-((5-(2-((4-methoxyphenyl)amino)ethyl)-4-phenyl-4H-1,2,4-triazol-3-yl)thio)ethanone has been identified as the most active compound against the glioblastoma U-87 cell line.

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23

Xu, Yan, Ran Dang, Jianguo Guan, Zhi Xu, Shijia Zhao, and Yuanqiang Hu. "Isatin-(thio)semicarbazide/oxime-1H -1,2,3-triazole-coumarin Hybrids: Design, Synthesis, and in vitro Anti-mycobacterial Evaluation." Journal of Heterocyclic Chemistry 55, no. 4 (February 12, 2018): 1069–73. http://dx.doi.org/10.1002/jhet.3104.

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24

Xu, Zhi, Xufeng Song, Yuanqiang Hu, Min Qiang, and Zaosheng Lv. "Design, Synthesis andIn VitroAnti-mycobacterial Activities of 8-OMe Ciprofloxacin-1H-1,2,3-triazole-isatin-(thio) Semicarbazide/Oxime Hybrids." Journal of Heterocyclic Chemistry 55, no. 1 (October 4, 2017): 192–98. http://dx.doi.org/10.1002/jhet.3024.

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25

Journal, Baghdad Science. "Synthesis and Characterization of 1,3,4-Oxadiazoles Derived From 9-Fluorenone." Baghdad Science Journal 10, no. 2 (June 2, 2013): 449–61. http://dx.doi.org/10.21123/bsj.10.2.449-461.

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In the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the corresponding 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole (8). Reaction of hydrazide (2) with phenyl isocyanate to give N-phenyl semicarbazide derivative (9), then this compound (9) convert to 5-(9-fluorenone-2-yl)-N-phenyl-1,3,4-oxadiazole-2-amine (10) via intramolecular cyclization by syrup H3PO4. Also the hydrazide (2) was treated with CS2/KOH afforded 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-thiol (11). Compound (11) was used to react with various alkyl halides and secondary amines to give 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-alkyl thiol (12-15) and 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-N-alkyl (16-19) derivatives respectively.

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26

Dawood, Rafid Saad. "Synthesis and Characterization of 1,3,4-Oxadiazoles Derived From 9-Fluorenone." Baghdad Science Journal 10, no. 2 (June 2, 2013): 449–61. http://dx.doi.org/10.21123/bsj.2013.10.2.449-461.

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In the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the corresponding 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole (8). Reaction of hydrazide (2) with phenyl isocyanate to give N-phenyl semicarbazide derivative (9), then this compound (9) convert to 5-(9-fluorenone-2-yl)-N-phenyl-1,3,4-oxadiazole-2-amine (10) via intramolecular cyclization by syrup H3PO4. Also the hydrazide (2) was treated with CS2/KOH afforded 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-thiol (11). Compound (11) was used to react with various alkyl halides and secondary amines to give 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-alkyl thiol (12-15) and 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-N-alkyl (16-19) derivatives respectively.

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27

Krátký, Martin, Šárka Štěpánková, Klára Konečná, Katarína Svrčková, Jana Maixnerová, Markéta Švarcová, Ondřej Janďourek, František Trejtnar, and Jarmila Vinšová. "Novel Aminoguanidine Hydrazone Analogues: From Potential Antimicrobial Agents to Potent Cholinesterase Inhibitors." Pharmaceuticals 14, no. 12 (November 26, 2021): 1229. http://dx.doi.org/10.3390/ph14121229.

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A series of thirty-one hydrazones of aminoguanidine, nitroaminoguanidine, 1,3-diaminoguanidine, and (thio)semicarbazide were prepared from various aldehydes, mainly chlorobenzaldehydes, halogenated salicylaldehydes, 5-nitrofurfural, and isatin (yields of 50–99%). They were characterized by spectral methods. Primarily, they were designed and evaluated as potential broad-spectrum antimicrobial agents. The compounds were effective against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus with minimum inhibitory concentrations (MIC) from 7.8 µM, as well as Gram-negative strains with higher MIC. Antifungal evaluation against yeasts and Trichophyton mentagrophytes found MIC from 62.5 µM. We also evaluated inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The compounds inhibited both enzymes with IC50 values of 17.95–54.93 µM for AChE and ≥1.69 µM for BuChE. Based on the substitution, it is possible to modify selectivity for a particular cholinesterase as we obtained selective inhibitors of either AChE or BuChE, as well as balanced inhibitors. The compounds act via mixed-type inhibition. Their interactions with enzymes were studied by molecular docking. Cytotoxicity was assessed in HepG2 cells. The hydrazones differ in their toxicity (IC50 from 5.27 to >500 µM). Some of the derivatives represent promising hits for further development. Based on the substitution pattern, it is possible to modulate bioactivity to the desired one.

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28

Silva, Bianca N. M., Policarpo A. Sales Junior, Alvaro J. Romanha, Silvane M. F. Murta, Camilo H. S. Lima, Magaly G. Albuquerque, Eliane D'Elia, et al. "Synthesis of New Thiosemicarbazones and Semicarbazones Containing the 1,2,3-1H-triazole-isatin Scaffold: Trypanocidal, Cytotoxicity, Electrochemical Assays, and Molecular Docking." Medicinal Chemistry 15, no. 3 (April 12, 2019): 240–56. http://dx.doi.org/10.2174/1573406414666180912120502.

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Background: Chagas disease, also known as American trypanosomiasis, is classified as one of the 17 most important neglected diseases by the World Health Organization. The only drugs with proven efficacy against Chagas disease are benznidazole and nifurtimox, however both show adverse effects, poor clinical efficacy, and development of resistance. For these reasons, the search for new effective chemical entities is a challenge to research groups and the pharmaceutical industry. Objective: Synthesis and evaluation of antitrypanosomal activities of a series of thiosemicarbazones and semicarbazones containing 1,2,3-1H triazole isatin scaffold. Method: 5&'-(4-alkyl/aryl)-1H-1,2,3-triazole-isatins were prepared by Huisgen 1,3-dipolar cycloaddition and the thiosemicarbazones and semicarbazones were obtained by the 1:1 reactions of the carbonylated derivatives with thiosemicarbazide and semicarbazide hydrochloride, respectively, in methanol, using conventional reflux or microwave heating. The compounds were assayed for in vitro trypanocidal activity against Trypanosoma cruzi, the aetiological agent of Chagas disease. Beyond the thio/semicarbazone derivatives, isatin and triazole synthetic intermediates were also evaluated for comparison. Results: A series of compounds were prepared in good yields. Among the 37 compounds evaluated, 18 were found to be active, in particular thiosemicarbazones containing a non-polar saturated alkyl chain (IC50 = 24.1, 38.6, and 83.2 &µM; SI = 11.6, 11.8, and 14.0, respectively). To further elucidate the mechanism of action of these new compounds, the redox behaviour of some active and inactive derivatives was studied by cyclic voltammetry. Molecular docking studies were also performed in two validated protein targets of Trypanosoma cruzi, i.e., cruzipain (CRZ) and phosphodiesterase C (TcrPDEC). Conclusion: A class of thio/semicarbazones structurally simple and easily accessible was synthesized. Compounds containing thiosemicarbazone moieties showed the best results in the series, being more active than the corresponding semicarbazones. Our results indicated that the activity of these compounds does not originate from an oxidation-reduction pathway but probably from the interactions with trypanosomal enzymes.

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29

Kalinina, V., Y. Gryzunov, N. Smolina, M. Uzbekov, E. Misionzhnik, and G. Dobretsov. "Disturbance of neurotransmitters monoamines and indices of reducing-oxidizing processes in patient with the first episode of schizophrenia (FES)." European Psychiatry 26, S2 (March 2011): 1412. http://dx.doi.org/10.1016/s0924-9338(11)73117-0.

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IntroductionEffective treatment of FES patients may lead to achievement of long-term remission, decrease the number of relapses and increase the level of social activity and quality of life.AimTo study some pathophysiological mechanisms of FES.MethodsThe group of patients who were investigated clinically and biochemically consists of 26 persons (11 women and 15 men, average age 28.2 ± 9.5 years) with the first psychotic episode (F20.0; F20.3). Some biochemical parameters, representing the monoaminergic systems, and some biophysical parameters, representing reducing-oxidizing processes, were investigated. These parameters in all patients were estimated following the admission and prior to any treatment.ResultsThe severity of the disorder on admission to the clinic according to PANSS score was 75,5 ± 2,2 (i.e., moderately severe). Patients with FES were characterized by a significant increase of platelet momnoamine oxidase activity (by 107%; р < 0,01) and decrease of serum semicarbazide-sensitive amine oxidase activity (by 29%; p < 0,001) in comparison to the controls. Both reactive capability of SH-group (Cys-34 residue) of serum albumin, the main source of thiols of plasma and intersticial fluid, measured in reaction with thiol-specific reagent - dithyonitrobenzoic acide, and kinetic coefficient were decreased in FES patients (by 24%; p = 0,02) in comparison to controls.ConclusionThese results show that FES patients are characterized by pronounced metabolic disturbances.

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Bhandarkar, Subodh, and Bhavana Khobragade. "Synthesis and Biological Study of 2-( 5-aryl-4,5-dihydro-1-substituted-pyrazol-3-yl )-Substituted-Naphthalene-1-Ol." Advanced Materials Research 1110 (June 2015): 306–10. http://dx.doi.org/10.4028/www.scientific.net/amr.1110.306.

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The literature survey reveals that pyrazoline derivatives have been studied extensively because of their ready accessibility, diverse chemical reactivity, broad spectrum of biological activity and variety of Industrial applications. Pyrazolines with sulphonamidoaryl substituent at 3-position show cerebroprotective, antidepressant activity , anti-implantation activity, hypoglycemic activity. Due to this vital biological roll of pyrazoline derivatives it was thought to synthesized titled pyrazolines. 2-Acetyl-1-naphthol is prepared by Modified Nenchi’s method which on treatment with furfuraldehyde and KOH gives 1-(1-hydroxy naphthalen-2-yl)-3-(furan-2-yl) prop-2-ene-1-ones in excellent yield. The chalcone when subjected to hydrazine / phenyl hydrazine/ semicarbazide / 2,4 dinitro phenyl hydrazine / isonicotinic acid hydrazide in DMF solvent to gives 3-(1-hydroxy naphthalene-2-yl)-5-(furan-2-yl)-1-substituted pyrazolines in 35-45% yield. All the melting points were taken in silicon oil bath with open capillary tubes and are uncorrected. 1 H NMR spectra were recorded on a Brucker AC300 FNMR spectrometer (300MHz), using TMS as an internal standard. IR spectra were recorded on a Nicolet-Impact 400 FT-IR spectrometer. Thin Layer Chromatography on silica gel-G, was used to check the purity of the compounds. Microanalysis of nitrogen was obtained on Colman 29-N analyzer. The synthesized compounds were characterized by elemental analysis, 1H NMR, IR Spectroscopy. All Newly synthesized compound were scanned for their antimicrobial and antifungal activity and all newly synthesized compounds shows an excellent antimicrobial and antifungal activities.

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PROKOF'EVA, A. F., ZH Z. SAPOZHNIKOVA, L. A. POKROVSKAYA, V. N. VOLKOVA, V. V. NEGREBETSKII, G. V. GOLOVKIN, and N. N. MEL'NIKOV. "ChemInform Abstract: Phosphorus-Containing Triazinylhydrazines and Triazinyl(thio)semicarbazides. Synthesis and Properties." ChemInform 20, no. 24 (June 13, 1989). http://dx.doi.org/10.1002/chin.198924218.

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"Synthesis and Evaluation of Antimicrobial Activities of New Functional Derivatives of 3-[5-(4-Nitrophenyl)-2-Furyl]-4-Pyrazole-Carbaldehydes." Biointerface Research in Applied Chemistry 11, no. 4 (January 2, 2021): 12159–69. http://dx.doi.org/10.33263/briac114.1215912169.

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The analysis of the biological potential of derivatives of 4-alkenyl- and imino functionalized pyrazoles is carried out, based on which the expediency of design of new structures with pharmacophore 5-(4-nitrophenyl)furanyl fragment is substantiated. Their synthesis method using a structural modification of 3-[5-(4-nitrophenyl)furan-2-yl]pyrazole-4-carbaldehyde to the corresponding alkenyl derivatives under the action of malononitrile, ethyl cyanoacetate, cyanoacetamide, and thioxoimidazolidine is proposed. The hydrazones, (thio)semicarbazones, and oximes were obtained by the condensation of corresponding aldehydes with hydrazides, (thio)semicarbazides, and hydroxylamine. The synthesized compounds' composition and structure were determined by elemental analysis, IR, and 1H NMR spectra. The fact existence of a mixture of E/Z-isomers among the series of obtained hydrazones of 1-phenyl-4-pyrazolecarbaldehydes was determined, and the quantitative ratio of geometric isomers was determined using 1H NMR spectroscopy data. The results of the microbiological evaluation of the synthesized pyrazole derivatives showed that they have a pronounced effect on strains of bacteria S. aureus ATCC 25923, E. coli ATCC 25922, and fungi of the genus Candida and are promising for the creation of effective antimicrobial agents.

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Panja, Anangamohan, Mainak Das, Narayan Ch Jana, Paula Brandão, Rosa Maria Gomila, Joaquin Ortega-Castro, Antonio Frontera, and Partha Pratim Ray. "Combined experimental and theoretical studies on a conformationally diverse (thio)semicarbazone based semiconducting materials." CrystEngComm, 2023. http://dx.doi.org/10.1039/d3ce00137g.

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This paper reports the synthesis and characterization of two closely related semicarbazone/thiosemicarbazone based organic compounds, N-(2-hydroxy-3-methoxy-5-methylbenzylidene)semicarbazide (1) and N-(2-hydroxy-3-methoxy-5-methylbenzylidene)thiosemicarbazide (2). Structural studies revealed the conformational diversity in these systems as...

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Gultekin, Ergün, Olcay Bekircan, Yakup Kolcuoğlu, and Atilla Akdemir. "Synthesis of new 1,2,4‐triazole–(thio)semicarbazide hybrid molecules: Their tyrosinase inhibitor activities and molecular docking analysis." Archiv der Pharmazie, April 26, 2021. http://dx.doi.org/10.1002/ardp.202100058.

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de Mello, Debora, Juliana Malavolta, Roberto Santos, Leonardo Lopes, Sidnei Moura, Darlene Flores, and Alex Flores. "Efficient Synthesis and Antimicrobial Activities of Long Alkyl Chain Trifluoromethyl1H-pyrazol-1-(thio)carboxamides and Trifluoromethyl-1H-pyrazol-1-yl-thiazoles." Journal of the Brazilian Chemical Society, 2021. http://dx.doi.org/10.21577/0103-5053.20200241.

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The synthesis of 3-alkyl-5-trifluoromethyl-1H-pyrazole-1-carboxamides, 3-alkyl5-trifluoromethyl-1H-pyrazole-1-thiocarboxamides, and 2-(3-alkyl-5-trifluoromethyl-1H-pyrazol1-yl)-thiazoles derivatives are reported. [3 + 2] cyclocondensations for a series of long alkyl chain 1,1,1-trifluoro-4-methoxyalk-3-en-2-ones and semicarbazide or thiosemicarbazide were carried out in ethanol, an eco-friendly medium. The series of trifluoromethyl-1H-pyrazol-1-ylthiocarboxamide following a [3 + 2] cyclocondensation with 2-bromoacetophenone were converted into two series of 2-(3-alkyl-5-trifluoromethyl-1H-pyrazol-1-yl)-thiazoles. Good yields (69-96%) of the isolated products were obtained. The structures of the new long alkyl chain 1H-pyrazoles and 2-(1H-pyrazol-1-yl)thiazoles were characterized using 1 H, 13C, and 19F nuclear magnetic resonance (NMR) spectroscopy and electrospray ionization tandem mass spectrometric (ESI MS/MS) data. Moreover, some of the products were evaluated for their antimicrobial activity against Gram-negative Escherichia coli American Type Culture Collection (ATCC) 35218, Salmonella enteritidis ATCC 13076, and Pseudomonas aeruginosa ATCC 15692; and Gram-positive Staphylococcus aureus ATCC 6538, methicillin resistant Staphylococcus aureus (MRSA clinical isolate), Streptococcus sp. (clinical isolate), and Candida albicans ATCC 14053 and Candida krusei ATCC 6258 fungi. All the tested 1H-pyrazoles exhibited antibacterial and antifungal activities at the tested concentrations. The compounds from series 4 were found to be powerful against MRSA.

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"THE UTILITY OF 1-CYANOACETYL-4-(4-ETHOXYPHENYL) THIO-SEMICARBAZIDE FOR SYNTHESIS OF PYRAZOLE, TRIAZOLE, THIAZOLE, PYRIDINE AND CHROMENE DERIVATIVES." Al-Azhar Bulletin of Science 22, Issue 1-A (June 1, 2011): 85–97. http://dx.doi.org/10.21608/absb.2011.7179.

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Al-Majidi, Suaad, M. H., Halah, A. R. Ibrahim, and Yasser, A. H. AL-issa. "Synthesis and Identification of Some New Derivatives of ([Benzyl Thio) Benzimidazole -N- (Methylene-5-Yl)] - 4,5- Di Substituted 1,2,4-Triazole and Evaluation of Their Activity as Antimicrobial and Anti-Inflammatory Agents." Iraqi Journal of Science, April 29, 2021, 1054–65. http://dx.doi.org/10.24996/ijs.2021.62.4.2.

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New 2-Mercaptobenzimidazole derivatives were synthesized. 4,5-disubsitituted 1,2,4-Triazole compounds 1b-2c were synthesized from 2-(benzylthio) benzimidazole compound a, which was then reacted with (NaH) in dioxane at a temperature of (0-5 C°) to produce the salt of compound a. Then the salt was reacted with ethyl chloro acetate to yield Ethyl 2-(benzylthio) benzimidazole acetate compound b. Compound b was converted to triazole derivatives by two pathways. The first pathway was reacting compound b with semicarbazide, thiosemicarbazide and phenylsemicarbazide in DMSO as a solvent to gain compounds 1b-3b, which were then cyclized by refluxed with 2N (NaOH) to yield 1,2,4-triazole derivatives compounds 4b-6b. The second pathway involved the treatment of compound b with hydrazine hydrate to produce N-acetohydrazide-2-(benzyl thio) benzimidazole c. Compound c was refluxed with carbon disulfide (CS2) in KOH alcoholic solution to obtain the salt compound 1c. The salt was treated with hydrazine hydrate to yield 1,2,4-triazole derivative compound 2c. The newly synthesized compounds b-2c were identified by FTIR, 1H-NMR and 13C-NMR and their physical properties were measured. Furthermore, their anti-microbial activities were tested against two Gram-positive and two Gram-negative bacteria and against one strain of fungi. Also, some of these synthesized compounds were tested for their anti-inflammatory activities.

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Hady, Ahmad Ayad, Mayada F. Darweesh, and Ahmad A. Motar. "The Antibacterial of Essential Fatty Acid Semicarbazide Extracted from Flaxseed Oil Against Some Nosocomial Infection Bacteria in Iraq." International Journal of Current Pharmaceutical Review and Research 8, no. 01 (February 25, 2017). http://dx.doi.org/10.25258/ijcprr.v8i01.9086.

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During the period from December 2014 to July 2015, isolation and identification of pathogenic bacteria from clinical sources attending to AL-Hakeem Hospital and AL-Sadder Medical City in AL-Najaf province. A total of One hundred clinical samples from various sources included: UTI - patients, Burn, postoperative surgery site –Wound, The results revealed the occurrence (52) bacterial isolate were isolated, 37(71%) were gram– positive bacteria that was divided into S. aureus 20(39%), S. pyogen 9 (17%), and S. pneumonia 8 (15%). But only 15 (29%) was gram – negative bacteria which represented by E. coli 7(13%), and P.aeruginasa 4 (8%), Protuse mirabilis 4(8%). The susceptibility of S. aureus and E.coli bacteria which are consider the most common G+ve and G-ve nosocomial pathogen to routenly used antibiotic in Najaf hospitals were tested by using antibiotic susceptibility pattrons, in order to select one isolate from S.aureus and other one from E.coli which had the higher resistance to most antibiotic for continue the other steps of these study. The result illustrated that S.aureus No.5 and E. coli No.3 were greatly resistant to antibiotics, so regard as multi-drug resistant(MDR). Crud extracts of Linum usitatissimum which had been extracted by three solvents (petroleum ether, hexan and aqueous), for studying the chemical contents of these extracts by using suitable reagents and tested antibacterial activity on the growth of studied S.aureus and E. coli bacteria. The extraction of Essential fatty acid Semicarbazide (omega-3-6- fatty acid) from Linum usitatissium (Flax seed) and the chemical and physical properties of isolated oil compounds were studied by using thin layer chromatography (TLC), ultraviolet spectrum (UV) and FTIR spectrum. The result revealed that shown high antibacterial activity against studied (S.aureus, E.coli). results explained broad spectrum antibacterial property of oil compounds against studied bacteria nosocomial.

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Jyothi, P., V. Sumalatha, and D. Rajitha. "Cobalt (II) complexes with N-methyl thio semicarbazide Schiff bases: Synthesis, Spectroscopic investigation, Cytotoxicity, DNA binding and incision, anti-bacterial and anti-fungal studies." Inorganic Chemistry Communications, September 2022, 110029. http://dx.doi.org/10.1016/j.inoche.2022.110029.

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