Journal articles: 'Aryl Compounds'

1

Wang, Xi-Cun, Fang Wang, Zheng-Jun Quan, Man-Gang Wang, and Zheng Li. "An efficient and clean synthesis of 1-aroyl-3-aryl-4-substituted imidazole-2-thiones in water." Journal of Chemical Research 2005, no. 11 (November 2005): 689–90. http://dx.doi.org/10.3184/030823405774909423.

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Treatment 1-aryl-3-aroyl/benzofuroyl thioureas with α-bromo substituted carbonyl compounds in water affording 1-aroyl/benzofuroyl-3-aryl-4-substituted imidazole-2-thiones in excellent yields within short time.

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Krutošíková, Alžbeta, Miloslava Dandárová, and Juraj Alföldi. "5-Aryl-2-furancarbaldehyde Hydrazones and Related Compounds." Collection of Czechoslovak Chemical Communications 58, no. 8 (1993): 1905–13. http://dx.doi.org/10.1135/cccc19931905.

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A series of 5-aryl-2-furancarbaldehyde 2,6-dialkylphenylhydrazones (Ia - Iv) and dimethylhydrazones (IIa - IIf) as well as related compound benzo[b]furan-2-carbaldehyde dimethylhydrazone (III) were prepared. Compounds Ia - Iv were synthesized by condensing 5-aryl-2-furancarbaldehydes with 2,6-dialkylphenylhydrazines, compounds IIa - IIf were obtained from the same starting compounds and N,N-dimethylhydrazine. The intermediate 5-aryl-2-furancarbaldehydes were prepared by reaction of aryldiazonium chlorides with 2-furancarbaldehyde. The structure of the compounds were proven by 1H, 13C and 15N NMR spectra.

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Soni, Love Kumar, Tamanna Narsinghani, and Rica Jain. "Synthesis and Antibacterial Screening of Some 1-Aroyl-3-aryl Thiourea Derivatives." ISRN Medicinal Chemistry 2014 (January 29, 2014): 1–6. http://dx.doi.org/10.1155/2014/393102.

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A series of 1-aroyl-3-aryl thioureas derivatives were synthesized and evaluated for antibacterial activity. The results indicated that the compounds possessed higher activity against gram-negative bacteria than gram-positive bacteria. Amongst all these compounds, C18 (89.4%) exhibited the greatest antibacterial activity against gram-negative bacteria while C5 (85.6%) displayed maximum antibacterial activity against gram-positive bacteria. Preliminary study of the structure-activity relationship revealed that an electronic factor on aryl rings had a great effect on the antibacterial activity of these compounds.

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Kalam, Sirisha, Rajyalaxmi I, and Olivia S. "Synthesis and In vitro P-Glycoprotein Inhibitory Activity of Novel 1,4-Dihydropyridine Derivatives." International Journal of Pharmaceutical Sciences and Nanotechnology 7, no. 3 (August 31, 2014): 2544–52. http://dx.doi.org/10.37285/ijpsn.2014.7.3.6.

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Two series of new symmetrical 4-aryl-2,6-dimethyl-3,5-bis-N-(aryl/heteroaryl)-carbamoyl-1,4-dihydropyridines (4a-f) and asymmetrical 4-aryl-2,6-dimethyl-3-N-(aryl/hetero-aryl)-carbamoyl-5-ethyl carboxylate-1,4-dihydro-pyridines (5a-f) have been synthesized by simple, economical and eco-friendly, modified Hantzsch reaction using N-aryl/heteroarylacetoacetamides (3a-c), ethylaceto-acetate (for asymmetric), arylaldehydes and urea in presence of catalytic amounts of LiBr/Iodine and by microwave irradiation methods. The newly synthesized compounds were characterized by physical and spectral data, and evaluated for their possible in vitro MDR reversal activity by everted sac method using verapamil as standard P-gp inhibitor and domperidone as the standard P-gp substrate. Amongst the compounds tested, compound 4f exhibited the highest in vitro P-gp inhibitory activity. It was found to be more potent than the standard verapamil.

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Raval, J. P., and K. R. Desai. "Synthesis of 3-Phenyl-4[4-(m-nitrophenyl)-N-2-(2’-arylureido / arylthioureido-4’-N-morpholino-s-triazin)-benzo-[6,7]-coumarins and their Applicatiions." E-Journal of Chemistry 1, no. 5 (2004): 211–15. http://dx.doi.org/10.1155/2004/873425.

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Several 3 – phenyl – 4 [4-(m– nitrophenyl) –N– 2 - (2’-arylureido /arylthioureido - 4’-N-morpholino-s-triazin)-benzo-(6,7)-coumarins were prepared using 2-(m–nitrophenyl)-3-hydroxy naphthalene, cyanuric chloride, morpholine and various aryl – ureas / aryl – thioureas derivatives to give desired compound. The structures of the compounds were confirmed by elemental analysis and spectral analysis. The antibacterial activities of these compounds have been screened and were also applied as Flourescent Brighteners on Polyester fabrics.

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Kudalkar, Gaurav P., Virendra K. Tiwari, Joshua D. Lee, and David B. Berkowitz. "A Hammett Study of Clostridium acetobutylicum Alcohol Dehydrogenase (CaADH): An Enzyme with Remarkable Substrate Promiscuity and Utility for Organic Synthesis." Synlett 31, no. 03 (January 16, 2020): 237–47. http://dx.doi.org/10.1055/s-0039-1691576.

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Described is a physical organic study of the reduction of three sets of carbonyl compounds by the NADPH-dependent enzyme Clostridium acetobutylicum alcohol dehydrogenase (CaADH). Previous studies in our group have shown this enzyme to display broad substrate promiscuity, yet remarkable stereochemical fidelity, in the reduction of carbonyl compounds, including α-, β- and γ-keto esters (d-stereochemistry), as well as α,α-difluorinated-β-keto phosphonate esters (l-stereochemistry). To better mechanistically characterize this promising dehydrogenase enzyme, we report here the results of a Hammett linear free-energy relationship (LFER) study across three distinct classes of carbonyl substrates; namely aryl aldehydes, aryl β-keto esters and aryl trifluoromethyl ketones. Rates are measured by monitoring the decrease in NADPH fluorescence at 460 nm with time across a range of substrate concentrations for each member of each carbonyl compound class. The resulting v 0 versus [S] data are subjected to least-squares hyperbolic fitting to the Michaelis–Menton equation. Hammett plots of log(V max) versus σX yield the following Hammett parameters: (i) for p-substituted aldehydes, ρ = 0.99 ± 0.10, ρ = 0.40 ± 0.09; two domains observed, (ii) for p-substituted β-keto esters ρ = 1.02 ± 0.31, and (iii) for p-substituted aryl trifluoromethyl ketones ρ = –0.97 ± 0.12. The positive sign of ρ indicated for the first two compound classes suggests that the hydride transfer from the nicotinamide cofactor is at least partially rate-limiting, whereas the negative sign of ρ for the aryl trifluoromethyl ketone class suggests that dehydration of the ketone hydrate may be rate-limiting for this compound class. Consistent with this notion, examination of the 13C NMR spectra for the set of p-substituted aryl trifluoromethyl ketones in 2% aqueous DMSO reveals significant formation of the hydrate (gem-diol) for this compound family, with compounds bearing the more electron-withdrawing groups showing greater degrees of hydration. This work also presents the first examples of the CaADH-mediated reduction of aryl trifluoromethyl ketones, and chiral HPLC analysis indicates that the parent compound α,α,α-trifluoroacetophenone is enzymatically reduced in 99% ee and 95% yield, providing the (S)-stereoisomer, suggesting yet another compound class for which this enzyme displays high enantioselectivity.

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7

Chandra, Priyanka, Swastika Ganguly, Rajdeep Dey, and Biswatrish Sarkar. "Synthesis, antibacterial activities, binding mode analysis and predictive ADME studies of novel 1-(aryl)-2-(1H-imidazol-1-yl)methanones." INTERNATIONAL JOURNAL OF PHARMACEUTICAL EDUCATION AND RESEARCH (IJPER) 2, no. 02 (December 30, 2020): 39–45. http://dx.doi.org/10.37021/ijper.v2i2.2.

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Introduction: In the present study a novel series of twelve 1-(aryl)-2-(1H-imidazol-1-yl)methanones 3(a-l) were synthesized and characterised by physicochemical and spectral analysis,viz. elemental analysis, IR spectroscopy, NMR spectroscopy. The antibacterial property of the compounds were examined, in order to develop new broad spectrum antibiotics. Methods: The compounds 3(a-l) were synthesised by reacting the corresponding 2-(aryl)-1H-imidazoles 2 with substituted benzoyl chlorides. Binding mode analysis of the most active compound was carried out. Predictive ADME studies were carried out for all the compounds. Results and Discussions: Among the synthesized compounds, (2-(3-nitrophenyl) (2,4-dichlorophenyl) -1Himidazol-1-yl)methanone 3i exhibited highest antibacterial activity. Binding mode analysis of the highest active compound was carried out in the active site of glucosamine-6-phosphate synthase (2VF5).

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8

Chandra, Priyanka, Swastika Ganguly, Rajdeep Dey, and Biswatrish Sarkar. "Synthesis, antibacterial activities, binding mode analysis and predictive ADME studies of novel 1-(aryl)-2-(1H-imidazol-1-yl)methanones." INTERNATIONAL JOURNAL OF PHARMACEUTICAL EDUCATION AND RESEARCH (IJPER) 2, no. 02 (December 30, 2020): 39–45. http://dx.doi.org/10.37021/ijper.v2i2.2.

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Introduction: In the present study a novel series of twelve 1-(aryl)-2-(1H-imidazol-1-yl)methanones 3(a-l) were synthesized and characterised by physicochemical and spectral analysis,viz. elemental analysis, IR spectroscopy, NMR spectroscopy. The antibacterial property of the compounds were examined, in order to develop new broad spectrum antibiotics. Methods: The compounds 3(a-l) were synthesised by reacting the corresponding 2-(aryl)-1H-imidazoles 2 with substituted benzoyl chlorides. Binding mode analysis of the most active compound was carried out. Predictive ADME studies were carried out for all the compounds. Results and Discussions: Among the synthesized compounds, (2-(3-nitrophenyl) (2,4-dichlorophenyl) -1Himidazol-1-yl)methanone 3i exhibited highest antibacterial activity. Binding mode analysis of the highest active compound was carried out in the active site of glucosamine-6-phosphate synthase (2VF5).

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9

Wang, Lizhong, Zhenjie Su, Siran Qian, Weijian Ye, and Cunde Wang. "Efficient Preparation of 2,3-Disubstituted Cyclopropane-1-Carbonitriles via Selective Decarboxylation of 1-Cyanocyclopropane-1-Carboxylates." Journal of Chemical Research 41, no. 11 (November 2017): 636–40. http://dx.doi.org/10.3184/174751917x15094552081161.

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2,3-Disubstituted cyclopropane-1-carbonitriles were efficiently formed via a selective decarboxylation reaction of substituted 2-aroyl-3-aryl-1-cyano-cyclopropane-1-carboxylates in up to 92% yield. The structures of three typical compounds were confirmed by X-ray crystallography.

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10

Utri, Gerhard, Karl-Eberhard Schwarzhans, and Günter M. Allmaier. "Ferrocenyl-aryl-plumbane / Ferrocenyl-aryl-plumbanes." Zeitschrift für Naturforschung B 45, no. 6 (June 1, 1990): 755–62. http://dx.doi.org/10.1515/znb-1990-0606.

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The first example of a diplumba[1.1]ferrocenophane[cpPb(ø2)cp]2Fe2 has been prepared from ø2PbCl2 and 1,1′-dilithioferrocene 2 TMEDA. The preparation of further four ferrocenyl-phenyl-plumbanes, including the hitherto unknown compounds (ø3Pbcp)2Fe, Fc2Pb2ø2 and [(ø3Pb)cpFecp]FcPbø2 has been achieved by reaction of a mixture of monolithioferrocene · TMEDA and 1,1′-dilithioferrocene 2 TMEDA with ø 2PbCl2 and ø3PbCl, respectively.These compounds have been investigated by 1H, 13C and 207Pb NMR spectroscopy as well as by half-wave potential measurements, EI, FD and PD mass spectrometry.The results were discussed in terms of the possibility of Pb/Fe metal orbital overlap.There is evidence from the VT 1H NMR spectra for conformational flexibility of the diplumba[ 1.1 ]ferrocenophane.

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11

Gudimani, Parashuram, Samundeeswari Lokesh Shastri, Varsha Pawar, Nagashree Uday Hebbar, Lokesh Anand Shastri, Shrinivas Joshi, Shyam Kumar Vootla, Sheela Khanapure, and Vinay Sunagar. "Synthesis, molecular docking, and biological evaluation of methyl-5-(hydroxyimino)-3-(aryl-substituted)hexanoate derivatives." European Journal of Chemistry 13, no. 2 (June 30, 2022): 151–61. http://dx.doi.org/10.5155/eurjchem.13.2.151-161.2220.

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Beta-aryl keto hexanoic acids (5a-l) were synthesized efficiently, followed by esterification that afforded beta-aryl keto methylhexanoates (6a-l). The chemo-selective ketoxime beta-aryl methyl hexanoates (7a-l) were isolated in good yields. Spectroscopic methods were used to characterize the obtained moieties. The antioxidant, anti-inflammatory, and antibacterial properties of the effectively synthesized compounds 7a-l were also investigated. The anti-inflammatory activity of the compounds 7c, 7f, 7i, and 7l was excellent, with a low IC50 value at micromolar concentration, which was much better than the reference diclofenac. All synthesized compounds 7a-l were assessed for their in vitro antibacterial activity against S. aureus, B. subtilis and E. coli. Most of the compounds exhibited promising activity against Gram-positive bacterial strain, compound 7i showed excellent activity compared to standard streptomycin and in the case of E. coli, compounds 7b, 7c, 7j, 7k and 7l have shown moderate activity. Further, the cytotoxic activities of the compounds were assessed against lung cancer cells (A549) by using MTT assay. The possible interaction mechanism of the molecules 7c and 7g with Gram-negative strain E. coli DNA gyrase B in complex with PDB ID: 4DUH was studied.

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12

Masri, Abdulkader, Ayaz Anwar, Naveed Ahmed Khan, Muhammad Saquib Shahbaz, Khalid Mohammed Khan, Syed Shahabuddin, and Ruqaiyyah Siddiqui. "Antibacterial Effects of Quinazolin-4(3H)-One Functionalized-Conjugated Silver Nanoparticles." Antibiotics 8, no. 4 (October 9, 2019): 179. http://dx.doi.org/10.3390/antibiotics8040179.

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Infections due to multi-drug resistant bacteria are on the rise and there is an urgent need to develop new antibacterials. In this regard, a series of six functionally diverse new quinazolinone compounds were synthesized by a facile one-pot reaction of benzoic acid derivatives, trimethoxymethane and aniline derivatives. Three compounds of 3-aryl-8-methylquinazolin-4(3H)-one, and 3-aryl-6,7-dimethoxyquinazolin4(3H)-one were prepared and tested against multi-drug resistant bacteria. Furthermore, we determined whether conjugation with silver nanoparticles improved the antibacterial efficacy of these quinazolinone derivatives. The newly synthesized compounds were characterized by ultraviolet visible spectrophotometry (UV-vis), Zetasizer analysis, Fourier transform infrared spectroscopic methods (FT-IR), and scanning electron microscopy (SEM). Using bactericidal evaluation, effects were determined against selected Gram-negative and Gram-positive bacteria. Furthermore, cytotoxicity of nanoconjugates on human cells were determined. The UV-vis spectrum of silver nanoparticles conjugated quinazolinone displayed surface plasmon resonance band in the range of 400–470 nm, and the size of nanoparticles was detected to be in the range of 100–250 nm by dynamic light scattering (DLS). FT-IR study confirmed the stabilization of silver nanoparticles by the presence of diverse functional arayl on each compound. SEM further revealed the construction of spherical nanoparticles. Among the quinazolinone derivative tested, two compounds (QNZ 4, QNZ 6) conjugated with silver nanoparticles showed enhanced antibacterial activity against Escherichia coli K1, Streptococcus pyogenes, Klebsiella pneumoniae, B. cereus and P. aeruginosa as compared to the compounds.

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13

Lan, Jihong, Rongxiang Chen, Fangfang Duo, Menghui Hu, and Xiaoyan Lu. "Visible-Light Photocatalytic Reduction of Aryl Halides as a Source of Aryl Radicals." Molecules 27, no. 17 (August 23, 2022): 5364. http://dx.doi.org/10.3390/molecules27175364.

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Aryl- and heteroaryl units are present in a wide variety of natural products, pharmaceuticals, and functional materials. The method for reduction of aryl halides with ubiquitous distribution is highly sought after for late-stage construction of various aromatic compounds. The visible-light-driven reduction of aryl halides to aryl radicals by electron transfer provides an efficient, simple, and environmentally friendly method for the construction of aromatic compounds. This review summarizes the recent progress in the generation of aryl radicals by visible-light-driven reduction of aryl halides with metal complexes, organic compounds, semiconductors as catalysts, and alkali-assisted reaction system. The ability and mechanism of reduction of aromatic halides in various visible light induced systems are summarized, intending to illustrate a comprehensive introduction of this research topic to the readers.

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14

Goyal, Anju, and Sandeep Jain. "Syntheses and Antibacterial Studies of Some 1-Phenyl-3-(4-(2-ethanoloxy) phenyl)-5-aryl-1H-pyrazoles." Journal of Chemistry 2013 (2013): 1–5. http://dx.doi.org/10.1155/2013/950491.

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A series of 1-phenyl-3-(4-(2-ethanoloxy) phenyl)-5-aryl-1H-pyrazoles were synthesized from chalcones, that is, 3-aryl-1-(4-hydroxyphenyl) prop-2-en-1-ones and studied for theirin vitroantibacterial activity. Chalcones1on reaction with phenyl hydrazine in the presence of acetic acid and few drops of hydrochloric acid yielded the corresponding 1-phenyl-3-(4-hydroxyphenyl)-5-aryl-1H-pyrazoles2which on further reaction with 2-chloroethanol furnished the title compounds3. These compounds were characterized by CHN analyses, IR, mass and1H NMR spectral data. All the compounds were evaluated for theirin vitroantibacterial activity against two Gram positive strains (Bacillus subtilisandStaphylococcus aureus) and two Gram negative strains (Escherichia coliandPseudomonas aeruginosa), and their minimum inhibitory concentration (MIC) was determined.

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15

FROHN, H. J. "ChemInform Abstract: Aryl-Xenon Compounds." ChemInform 25, no. 6 (August 19, 2010): no. http://dx.doi.org/10.1002/chin.199406285.

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Al-Khazragie, Zainab K., Bushra K. Al-Salami, and Adnan J. M. Al-Fartosy. "Synthesis, Characterization, and Antioxidant, Antimicrobial and Toxic Properties of Novel Δ2 -1,3,4-thiadiazoline and Δ2 -1,3,4-selenadiazoline Derivatives." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, no. 01 (June 25, 2022): 113–26. http://dx.doi.org/10.25258/ijddt.12.1.22.

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Two new series of N-(4-acetyl-5-aryl-4,5-dihydro-1,3,4-thiadiazol-2-yl)acetamide and N-(4-acetyl-5-aryl-4,5-dihydro1,3,4-selenadiazol-2-yl)acetamide compounds (where aryl = 4-nitrophenyl, 4-hydroxy-3-methoxyphenyl, 3-ethoxy-4- hydroxyphenyl, 2-chloroquinolinyl, and 6-chloro-4-oxo-4H-chromenyl) were synthesized in good yields by heterocyclization of thiosemicarbazones (TSCs) and selenosemicarbazones (SSCs) with acetic anhydride, respectively. The new TSCs and SSCs compounds was prepared by condensation reaction of thiosemicarbazide and Selenosemicarbazide with aromatic aldehydes in acidic medium. The structures of newly synthesized 1,3,4-thiadiazoline (TDZs) and 1,3,4-selenadiazoline (SDZs) derivatives were characterized by the analytical and spectroscopic method such as IR, 1 H NMR, 13C NMR, mass spectra and elemental analysis. The purity of compound and evaluation of Rf value were determined by TLC. The toxicity of new compounds was assayed via the determination of their LD50 value by using Dixon’ s up and down method. The antibacterial activity of 1,3,4-thiadiazoline and 1,3,4-selenadiazoline compounds were tested in vitro against Staphylococcus aureus, Bacillus, Escherichia coli and Pseudomonas aeruginosa. Finally, antioxidant efficiency of all compounds were detected according to β-carotene bleaching method.

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17

Mete, Ebru, Halise Inci Gul, Pakize Canturk, Zeki Topcu, Bulbul Pandit, Mustafa Gul, and Pui-Kai Li. "Biological Activity of 1-Aryl-3-phenethylamino-1-propanone Hydrochlorides and 3-Aroyl-4-aryl-1-phenethyl-4-piperidinols on PC-3 Cells and DNA Topoisomerase I Enzyme." Zeitschrift für Naturforschung C 65, no. 11-12 (December 1, 2010): 647–52. http://dx.doi.org/10.1515/znc-2010-11-1203.

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1aA number of studies reported Mannich bases to manifest antimicrobial, cytotoxic, anticancer, anti-inflammatory, and anticonvulsant activities. A considerable number of therapeutically important cytotoxic compounds are active on DNA topoisomerases that regulate the DNA topology. In the present study we evaluated the biological activity of mono- Mannich bases, 1-aryl-3-phenethylamino-1-propanone hydrochlorides (- 10a), and semicyclic mono- Mannich bases, 3-aroyl-4-aryl-1-phenethyl-4-piperidinols (1b - 9b), synthesized in our laboratory. We employed androgen-independent human prostate cancer cells (PC-3) to assess the cytotoxicity of the compounds and extended the biological activity evaluation to cover supercoil relaxation assays of mammalian type I topoisomerases. Our results showed that the compounds had cytotoxicity within the 8.2 - 32.1 μM range, while two compounds gave rise to a comparable average value in topo I interference of 42% and 40% for 10a (with a hydroxy substituent on the phenyl ring from mono-Mannich bases) and 5b (with a fluoro substituent on the phenyl ring from the semicyclic mono-Mannich base series, piperidinols), respectively

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18

Little, Vanessa Renee, and Keith Vaughan. "Synthesis and characterization of several series of 4-acyl-1-[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 92, no. 9 (September 2014): 838–48. http://dx.doi.org/10.1139/cjc-2014-0242.

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Five series of a novel class of 4-acyl-1-[2-aryl-1-diazenyl]piperazines have been synthesized and characterized: the 4-acetyl-1-[2-aryl-1-diazenyl]piperazines [series 1]; the 4-cyclohexylcarbonyl-1-[2-aryl-1-diazenyl]piperazines [series 2]; the 4-benzoyl-1-[2-aryl-1-diazenyl]piperazines [series 3]; the benzyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 4]; and the t-butyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 5]. The compounds were synthesized by diazotization of a primary aromatic amine and subsequent coupling to an appropriate secondary amine: 1-acetylpiperazine [series 1]; 1-(cyclohexylcarbonyl)-piperaizine [series 2]; 1-benzoylpiperazine [series 3]; benzyl 1-piperazinecarboxylate [series 4]; and t-butyl piperazine-1-carboxylate (1-BOC-piperazine) [series 5]. The compounds of series 1–5 were characterized by 1H NMR, 13C NMR, high-resolution MS and IR spectroscopy. The model compounds 1,4-di[2-aryl-1-diazenyl]piperazines, and ethyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates were used to facilitate the assignment of the chemical shifts specific to the piperazine ring carbons. HSQC spectra of select compounds established the correlation between proton and carbon resonance signals.

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Ogorodnik, A. G., V. A. Yanchenko, L. S. Bobkova, N. M. Seredinska, and A. M. Demchenko. "Synthesis and anаlgеsic activity 5-methyl-3-aryl[1,2,4]triazolo[4,3-a]pyrimidin-7-oles derivatives." Farmatsevtychnyi zhurnal, no. 2 (August 14, 2018): 55–61. http://dx.doi.org/10.32352/0367-3057.2.17.07.

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Pain is a signal of inflammation and disruption of the body. It is the most important protective and adaptive mechanism that ensuring the safety of the individual. A strong and prolonged effect of "pain" irritant arising in injuries or after surgical manipulation transforms the protective reaction of the body to harmful factor that is the cause of secondary violations physiological processes. The aim of this work was the synthesis of substances in a series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol and study the analgesic effect of the synthesized compounds. The objects of our research were selected derivatives of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol, which were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanilpirymidyn-4-ol (1) with the corresponding substituted benzoic acid hydrazide The primary evaluation of analgesic activity conducted on thermal stimulation models («hot plate»). A number of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives were synthesized, and their structure and purity were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship. The screening for analgesic activity for 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives in in vivo experiments on hot plate models showed that the highest activity Was noted for the compound containing the methyl group in the fourth position of the aryl substituent, which is 184.28% of the change in the latent period of the reaction, which exceeds the action of the reference preparation of ketorolac by 71.57%. The introduction of halogens into the aryl moiety leads to a decrease in the analgesic activity of the compounds. A series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol derivatives were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanylpirymydyn-4-ol with relevant substituted hydrazide of benzoic acid. The structure and purity of obtained compounds were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship. The screening of analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pirymidyn-7-ol derivatives in vivo models for «hot plate» shows that the highest activity was noted for compound containing methyl group in the fourth position of the aryl substituent, which is 184.28% change latent period reaction, that exceeds effect reference drug ketorolac at 71.57%. The introduction of halogens in the aryl fragment leads to a decrease analgesic activity of compounds.

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Peeters, Elien, Geert Hooyberghs, Stijn Robijns, Kai Waldrant, Ami De Weerdt, Nicolas Delattin, Veerle Liebens, et al. "Modulation of the Substitution Pattern of 5-Aryl-2-Aminoimidazoles Allows Fine-Tuning of Their Antibiofilm Activity Spectrum and Toxicity." Antimicrobial Agents and Chemotherapy 60, no. 11 (August 22, 2016): 6483–97. http://dx.doi.org/10.1128/aac.00035-16.

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ABSTRACTWe previously synthesized several series of compounds, based on the 5-aryl-2-aminoimidazole scaffold, that showed activity preventing the formation ofSalmonella entericaserovar Typhimurium andPseudomonas aeruginosabiofilms. Here, we further studied the activity spectrum of a number of the most activeN1- and 2N-substituted 5-aryl-2-aminoimidazoles against a broad panel of biofilms formed by monospecies and mixed species of bacteria and fungi. AnN1-substituted compound showed very strong activity against the biofilms formed by Gram-negative and Gram-positive bacteria and the fungusCandida albicansbut was previously shown to be toxic against various eukaryotic cell lines. In contrast, 2N-substituted compounds were nontoxic and active against biofilms formed by Gram-negative bacteria andC. albicansbut had reduced activity against biofilms formed by Gram-positive bacteria. In an attempt to develop nontoxic compounds with potent activity against biofilms formed by Gram-positive bacteria for application in antibiofilm coatings for medical implants, we synthesized novel compounds with substituents at both theN1 and 2Npositions and tested these compounds for antibiofilm activity and toxicity. Interestingly, most of theseN1-,2N-disubstituted 5-aryl-2-aminoimidazoles showed very strong activity against biofilms formed by Gram-positive bacteria andC. albicansin various setups with biofilms formed by monospecies and mixed species but lost activity against biofilms formed by Gram-negative bacteria. In light of application of these compounds as anti-infective coatings on orthopedic implants, toxicity against two bone cell lines and the functionality of these cells were tested. TheN1-,2N-disubstituted 5-aryl-2-aminoimidazoles in general did not affect the viability of bone cells and even induced calcium deposition. This indicates that modulating the substitution pattern on positionsN1 and 2Nof the 5-aryl-2-aminoimidazole scaffold allows fine-tuning of both the antibiofilm activity spectrum and toxicity.

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Raied, Mustafa Shakir, Abed Saoud Shaimaa, Faruk Hussain Dhuha, Fahad Ali Khalid, Shawqi Algburi Firas, and Salman Jasim Husam. "Synthesis, Antioxidant ability and Docking study for new 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))diphenol)." Research Journal of Chemistry and Environment 26, no. 10 (September 25, 2022): 28–36. http://dx.doi.org/10.25303/2610rjce028036.

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New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for the aryl attached position two for benzimidazole decrease the capability of interaction and give less bending and smaller docking score and there is inverse relationship between increasing hindrances around phenolic hydroxyl and DNA polymerase inhibition for these compounds.

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Nancy, Sakshi Chaudhary, Deepak Kumar, and Archana. "Synthesis and Anti-inflammatory Activity of Newer Indolyl Pyrazolines and Indolyl Isoxazolines." Asian Journal of Organic & Medicinal Chemistry 7, no. 1 (2022): 79–83. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p365.

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Various 5-substituted aryl-3-(2′-carboxy-5′-methoxyindolyl)-2-pyrazolines (9-15) and 5-substituted aryl-3-(2′-carboxy-5′-methoxyindolyl)isoxazolines (16-22) have been synthesized by the cyclization of compounds 1-(2′-carboxyl-5′-methoxyindolyl-3-arylidenyl chalcones (2-8) by treating them with hydrazine hydrate/glacial acetic acid and hydroxylamine hydrochloride/2% NaOH, respectively and TLC checked for their purity. Structure of all these newly synthesized compounds was characterized by elemental (C, H, N) analysis and IR and 1H NMR spectroscopy. All the synthesized compounds were tested for their anti-inflammatory and ulcerogenic activities and acute toxicity and found to possess varying degrees of these activities. Compound 15 is 5-(3′′-methoxy-4′′-hydroxyphenyl)-3- (2′-carboxy-5′-methoxyindolyl)-2-pyrazoline found to be the most potent compound of the series, more potent than the standard drug phenylbutazone.

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Rawat, Bhupender Singh, and S. C. Mehra. "SYNTHESIS OF SOME NEW 1, 3-DI METHYL SUBSTITUTED GUANIDINE WITH POSSIBLE ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY." Green Chemistry & Technology Letters 2, no. 3 (June 26, 2016): 138–40. http://dx.doi.org/10.18510/gctl.2016.233.

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The compounds containing thiazole, thiadiazole, oxazole, oxadiazole, imidazole, pyrimidine, pyridine & benzothiazole rings have been found to exhibit broad spectrum of biological activities.Derivatives of 1, 2, 4-thiadiazole and 1, 2, 4-thiadiazolidines exhibit antibacterial and antifungal activity1. Thiazolyl guanidines2 and various substituted aryl guanidine’s have been found to exhibit antibacterial & antifungal activities3.Keeping all these views in mind attempts were made to synthesized some new 1,3-di methyl Substituted Guanidine.In the present work 2,4 Dimethyl -3,5-(di Aryl imino)-1,2,4-thiadiazolidines were prepared by nitrous acid oxidation of N-methyl –N Aryl thiourea4 & 2,4 dimethyl-3,5-(diaryl imino)-1,2,4-thiazolidines were converted to corresponding 1,3 di methyl substituted guanidine’s by their acid catalyzed re-arrangment5.(Scheme-1)Antibacterial & Antifungal activity of the title compounds were evaluated against two bacteria, E.coli & lactobacillus & two fungi, A.Brassicicola & Aspergillus Niger. N=methyl-N`-Aryl thiourea (1-10) were prepared by refluxing a mixture of different 2-Amino Heterocyclic moieties with methyl iso thiocyanate in Ethanol.A mixture of compound (1-100 and conc. HCl, ethanol was added drop wise & under stirring to a solution of NaNO2 in water afforded 2, 4-dimethyl-3,5-(di Aryl imino)-1,2,4-thiadiazolidine (11-20) afforded 1,3 di methyl substituted guanidine’s (21-30). Structures of the compounds were established by elemental analysis & spectral data.

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Adachi, Ryutaro, Tsuyoshi Ishii, Shinichi Matsumoto, Takuya Satou, Junichi Sakamoto, and Tomohiro Kawamoto. "Discovery of Human Intestinal MGAT Inhibitors Using High-Throughput Mass Spectrometry." SLAS DISCOVERY: Advancing the Science of Drug Discovery 22, no. 4 (October 8, 2016): 360–65. http://dx.doi.org/10.1177/1087057116673181.

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Monoacylglycerol acyltransferase (MGAT) activity catalyzes the synthesis of diacylglycerol (DAG) from fatty acyl-CoA and monoacylglycerol as substrates. It is important for the resynthesis of triacylglycerol (TAG) in the intestine. In the present study, we developed a MGAT enzymatic assay of human intestinal microsomes using a high-throughput mass spectrometry (MS)–based detection system. After screening with small-molecular-weight libraries for compounds exhibiting inhibitions against DAG and the consequent TAG syntheses, we identified multiple compounds that specifically inhibit intestinal MGAT activity. The inhibitory activities of these compounds were correlated to those determined using a recombinant human MGAT2 enzyme. An aryl-sulfonamide compound T1 showed potent inhibitory activity toward human intestinal MGAT and recombinant human MGAT2, with selectivity over MGAT3. This high-throughput MS-based assay provides a novel platform for the discovery of DAG or TAG synthesis inhibitors. The identified aryl-sulfonamide compound T1 is a promising starting compound for optimization studies of inhibitors with selectivity toward MGAT2.

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Yao, Yun-Xin, Nan-Nan Jia, Ya-Nan Cao, Xing-Xiu Chen, Feng Gao, and Xiao-Xia Liang. "Copper-Catalyzed Synthesis, Bio-Evaluation, and in Silico Studies of 2-Aryl-N-alkylbenzimidazoles as Neuroprotective Agents." Catalysts 8, no. 10 (September 30, 2018): 433. http://dx.doi.org/10.3390/catal8100433.

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2-aryl-N-alkylbenzimidazole derivatives synthesized by CuI/PPh3 promoted direct coupling of N-alkylbenzimidazoles with aryl bromides. In vitro neurotoxicities of 20 compounds were evaluated, and the neuroprotective abilities of low-neurotoxic compounds (3b, 3g, 3h, 3i, 3j, 3k, 3o, 3q, 3s and 3t) were investigated against toxicity induced by 1-methyl-4-phenylpyridinium ion (MPP+) in SH-SY5Y neuronal cells. In silico studies revealed that compound 3g could have molecule docking with the following proteins: the bone morphogenetic protein receptor type 1B (BMPR1B), human cytochrome P450 1B1(CYP1B1), Metabotropic glutamate receptor 7 (GRM7), histone deacetylase 6 (HDAC6), 5-hydroxytryptamine receptor 5A (HTR5A), human topoisomerase II beta (TOP2B). A molecular docking simulation of model compound 3g and model protein CYP1B1 has been shown.

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26

Singh, A. "SYNTHESIS OF NOVEL QUINAZOLIN-4(3H)-ONYL AZETIDINONES AS POTENTIAL ANTICONVULSANT AGENTS." INDIAN DRUGS 54, no. 11 (November 28, 2017): 22–27. http://dx.doi.org/10.53879/id.54.11.10766.

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A series of 4-(substituted aryl)- 1- [2’- methyl-6’- substituted anilino quinazolinon-4’-(3’H)-onyl ] -3- chloroazetidin- 2-ones 14-25 have been synthesized by addition of substituted anilines to 4-(substituted aryl)- 1- [2’- methyl-6’- bromoquinazolinon-4’-(3’H)-onyl ] -3- chloro- azetidin-2-ones 8-13 which in turn were prepared by the cycloaddition of triethylamine in dioxane to 3-(N-substituted benzylidene amino phenyl amido )-2-methyl-6-bromoquinazolin-4(3H)-ones 2-7 in presence of acetyl chloride. These compounds were screened for anticonvulsant activity and acute toxicity. Compound 4-(substituted aryl)- 1- [2’- methyl-6’- substituted anilino quinazolinon-4’-(3’H) – onyl ] -3- chloro-azetidinone showed most potent activity. The structure of all the synthesized compounds were delineated by elemental (C, H, N ) and spectra (IR, proton magnetic resonance and mass ) analysis.

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Jaradat, Nidal, Mohammed Hawash, and Murad Abualhasan. "Synthesis and Biological Evaluation of Benzodioxol Derivatives as Cyclooxygenase Inhibitors." Letters in Drug Design & Discovery 17, no. 9 (September 11, 2020): 1117–25. http://dx.doi.org/10.2174/1570180817999200420114402.

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Background: Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely used therapeutics; they are competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the conversion of arachidonic acid to inflammatory prostaglandins. Objective: In this study, new benzodioxol derivatives with different core cycles and functional groups (i.e., aryl acetate, aryl acetic acid and diazepine) were designed, synthesized, identified and evaluated for their analgesic and anti-inflammatory activity, as a preliminary screening study to identify the most potent and more selective groups. Methods: The synthesized compounds were identified using FTIR, HRMS, 1H-NMR and 13C-NMR, and evaluated for their inhibitory activity against ovine COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay kit. Results: Six compounds were synthesized as a preliminary screening study to identify which was the most potent and more selective group towards COX-2 versus COX-1, compared to ketoprofen as non-selective NSAIDs. The compounds have three different groups: aryl acetate, aryl acetic acid and diazepine. The results showed that the most potent compound against the COX- 1 enzyme was 4b (which has diazepine and 2-chlorophenyl) with IC50 = 0.363 μM, and the selectivity ratio of 4b was found to be better than ketoprofen. In contrast, compound 4a (which has diazepine and 3-chlorophenyl) was the most selective with a COX-1/COX-2 ratio value of 0.85 in comparison with a ketoprofen ratio value of 0.20. Conclusion: In general, the synthesized library has moderate activity against both enzymes (i.e., COX-1 and COX-2). Moreover, all six compounds have better COX-2 inhibition selectivity compared to the commercial drug ketoprofen.

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Heidari, Alireza. "Interaction between Cadmium Oxide (CdO) Nanoparticles Aggregation Linked to DNA/RNA and Aryl Mercaptanes With Various Chain Length." Academic Journal of Chemistry, no. 72 (April 28, 2022): 23–29. http://dx.doi.org/10.32861/ajc.72.23.29.

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CdO nanoparticles show a strong peak of Plasmon absorption in ultraviolet–visible zone. A strong interaction exists between the surface of CdO nanoparticles and aryl mercaptan compounds. Aryl mercaptan compounds cause aggregation of CdO nanoparticles linked to DNA/RNA and hence, lead to widening of peak Plasmon of CdO nanoparticles surface at 550 (nm) and emerging a new peak at a higher wavelength. In the current project, this optical characteristic of CdO nanoparticles is used to time investigate of interaction between different aryl mercaptanes and CdO nanoparticles. The results were shown that aryl mercaptan compounds with shorter chain length interact faster with CdO nanoparticles. Therefore, a simple and fast method for identification of aryl mercaptanes with various chain length using red shift in surficial Plasmon absorption is presented. Schematic of Cadmium Oxide (CdO) Nanoparticles Aggregation Linked to DNA/RNA by Aryl Mercaptanes with Various Chain Length.

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29

Wanare, Rajendra K., Yogesh V. Punatkar, and Ravin M. Jugade. "SYNTHESIS, POLAROGRAPHIC AND ANTIMICROBIAL STUDIES OF BENZISOXAZOLYLN- GLUCOSIDES." Journal of Advanced Scientific Research 12, no. 04 Suppl 1 (December 31, 2021): 281–87. http://dx.doi.org/10.55218/jasr.s1202112432.

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The desired compounds 7-amino-3-methyl-5-(3′-aryl prop-2′-enoyl)-1,2-benzisoxazoles 2a-j were prepared by the reaction of appropriate 5-acetyl-7-amino-3-methyl-1,2-benzisoxazole 1 with different aromatic aldehydes. The reaction of (2a-j) with hydroxylamine hydrochloride was done to form 7-amino-3-methyl-5-(3′-aryl isoxazol-5′-yl)-1,2- benzisoxazoles (3a-j). Condensation of tetra-O-acetyl-α-D-glucopyranosyl bromide (TAGBr) with 7-amino-3-methyl-5- (3′-aryl isoxazol-5′-yl)-1,2-benzisoxazoles furnishes 7-amino-(β-D-2,3,4,6-tetra-O-acetyl glucopyranosyl)-3-methyl-5- (3′-aryl isoxazol-5′-yl)-1,2-benzisoxazoles (4a-j) which on deprotection yielded 7-amino-(β-D-glucopyranosyl)-3- methyl-5-(3′-aryl isoxazol-5′-yl)-1,2-benzisoxazoles (5a-j). The identities of newly synthesized compounds were established on the basis of IR, 1HNMR, 13CNMR, Mass spectral, Elemental analysis, TLC, and Polarographic studies. All compounds have been evaluated for antimicrobial activities and some compounds show potent activities.

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Bhat, Mashooq Ahmad, Ahmad M. Naglah, Azmat Ali Khan, and Abdullah Al-Dhfyan. "Synthesis, molecular modelling and antibacterial activity of 4-aryl-thiosemicarbazides." Polish Journal of Chemical Technology 24, no. 1 (March 1, 2022): 39–46. http://dx.doi.org/10.2478/pjct-2022-0006.

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Abstract N-Substituted phenyl/cyclohexyl-2-(pyridine-4-carbonyl) hydrazine-1-carbothioamides (2a–r) were synthesized, characterized by spectral and analytical data. The compounds were evaluated for antibacterial activity by the disc diffusion method. Most of the compounds showed activity against Gram-positive bacteria. Compound 2h with 4-Sulfapyrimidine phenyl substitution was found to be the most promising candidate, active against Gram-positive and methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentration (MIC) of (2–7 μg/mL). From the docking study, we predicted that compounds (2r, 2g, 2h, 2o, 2p and 2e) possess better antibacterial activity by having a good binding affinity with target protein and they could be used as potential drugs as antimicrobials. Amongst all the docked compounds, the compound 2h presented near binding affinity & interaction docking score with DNA gyrase enzymes with reference to ciprofloxacin.

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31

Heidari, Alireza. "Biomedical and Biochemical Approaches and Strategies for Targeting and Delivery of Cadmium Oxide (CdO) Nanoparticles Aggregation Linked to DNA/RNA by Aryl Mercaptanes with Various Chain Length." Biomedicine and Chemical Sciences 1, no. 4 (October 1, 2022): 215–24. http://dx.doi.org/10.48112/bcs.v1i4.149.

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CdO nanoparticles show a strong peak of Plasmon absorption in ultraviolet-visible zone. A strong interaction exists between the surface of CdO nanoparticles and aryl mercaptan compounds. Aryl mercaptan compounds cause to aggregation of CdO nanoparticles linked to DNA/RNA and hence, lead to widening of peak Plasmon of CdO nanoparticles surface at 550 (nm) and emerging a new peak at higher wavelength. In the current project, this optical characteristic of CdO nanoparticles is used to time investigate of interaction between different aryl mercaptanes and CdO nanoparticles. The results were shown that aryl mercaptan compounds with shorter chain length interact faster with CdO nanoparticles. Therefore, a simple and fast method for identification of aryl mercaptanes with various chain length using red shift in surficial Plasmon absorption is presented.

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32

Heidari, Alireza. "A New Viewpoint and Outlook on Aryl Mercaptans as Strong Nucleophiles with Various Chain Length Linked to DNA/RNA and Cadmium Oxide (CdO) Nanoparticles Sandwiched Complex." Asian Journal of Engineering and Applied Technology 10, no. 2 (November 5, 2021): 34–38. http://dx.doi.org/10.51983/ajeat-2021.10.2.3073.

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CdO nanoparticles show a strong peak of Plasmon absorption in ultraviolet–visible zone. A strong interaction exists between the surface of CdO nanoparticles and aryl mercaptan compounds. Aryl mercaptan compounds cause to aggregation of CdO nanoparticles linked to DNA/RNA and hence, lead to widening of peak Plasmon of CdO nanoparticles surface at 550 (nm) and emerging a new peak at higher wavelength. In the current project, this optical characteristic of CdO nanoparticles is used to time investigate of interaction between different aryl mercaptanes and CdO nanoparticles. The results were shown that aryl mercaptan compounds with shorter chain length interact faster with CdO nanoparticles. Therefore, a simple and fast method for identification of aryl mercaptanes with various chain length using red shift in surficial Plasmon absorption is presented.

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33

Claridge, Robert P., Ross W. Millar, John P. B. Sandall, and Claire Thompson. "Preparation of a Series of N-Aryl-S,S-diphenylsulfilimines by Nucleophilic Attack of S,S-Diphenyl-sulfilimine on Activated Halogenoaromatic Compounds." Journal of Chemical Research 23, no. 8 (August 1999): 520. http://dx.doi.org/10.1177/174751989902300833.

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Some N-aryl- S,S-diphenylsulfilimines, most of which are novel compounds, are prepared and characterised, using a method based on nucleophilic attack of diphenylsuifilimine on activated aryl halides, especially polyhalogenated heterocyclic aromatic compounds.

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34

Ashok, D., and K. Aravind. "Microwave Assisted Synthesis of New 1-{2, 4-Dihydroxy-5-[5-(aryl)-1-pyridine/pyrimidine-4-carbonyl)-4, 5-dihydro-1H-pyrazol-3-yl]-phenyl}-3-(aryl)-propenones and their Antibacterial Activity." E-Journal of Chemistry 6, no. 2 (2009): 323–31. http://dx.doi.org/10.1155/2009/982746.

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A series of 1-{2, 4-dihydroxy-5-[5-(aryl)-1-pyridine/pyrimidine-4-carbonyl)-4, 5-dihydro-1H-pyrazol-3-yl]-phenyl}-3-(aryl)-propenones (2a-h) have been synthesized from 1-[2,4-dihydroxy-5-(aryl acryloyl)phenyl]-aryl propenones(1a-h)by Micheal addition with isoniazide/pyrazinic acid hydrazide under microwave irradiation and classical heating. The synthesized compounds were characterized by IR,1H-NMR,13C-NMR and Mass spectral data. All the compounds were screened for their Antibacterial activity.

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35

Ma, Shuchao, Ben Ouyang, Linan Wang, and Lei Yao. "Design and Biological Evaluation of 3-Aryl-4-alkylpyrazol-5-amines Based on the Target Fishing." Current Computer-Aided Drug Design 16, no. 5 (November 9, 2020): 564–70. http://dx.doi.org/10.2174/1573409915666191003123900.

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Background: Pyrazol-5-amine derivatives are an important class of heterocyclic compounds. However, there are less 4-alkyl substituted pyrazoles reported. Objective: Here reported are the design, synthesis and biological evaluation of 3-aryl-4- alkylpyrazol-5-amines derivatives. Methods: A serials of 3-aryl-4-alkylpyrazol-5-amines were designed and the biological action targets were screened by target fishing function of Discovery Studio software. The synthesis route involved 3-oxo-3-arylpropanenitrile formation, alkylation, pyrazole formation, and amides formation. The antitumor activities of these compounds were carried out by thiazolyl blue tetrazolium bromide (MTT) method using U-2 OS (osteosarcoma) and A549 (lung cancer) tumor cells. Results: Eight 3-aryl-4-alkylpyrazol-5-amines were synthesized, and their structures were verified by 1H NMR, 13C NMR, and HRMS. Thirteen pharmacophores were mapped out by target fishing. Compound 5h showed anti-proliferation activities against U-2 OS and A549 tumor cell with IC50 value of 0.9 μM and 1.2 μM, respectively. Conclusion: Compound 5h might represent a promising scaffold for the further development of novel antitumor drugs.

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36

Macaev, Fliur. "What Can Be Done with the Acetyl Group of Aryl-1-Ethanones?" Chemistry Journal of Moldova 1, no. 1 (December 2006): 36–49. http://dx.doi.org/10.19261/cjm.2006.01(1).10.

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Literature data on utilization of acetyl group of aryl-1-ethanones (acetophenones) for the synthesis of organic compounds is generalized. Different approaches of preparation of aromatic compounds by chemical transformations of methyl as well as keto- group of titled compounds are systematized. Examples of the synthesis of organic compounds based on products of primary transformations of aryl-1-ethanones are considered.

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37

Nagaki, Aiichiro, and Yosuke Ashikari. "Homogeneous Catalyzed Aryl–Aryl Cross-Couplings in Flow." Synthesis 53, no. 11 (January 18, 2021): 1879–88. http://dx.doi.org/10.1055/a-1360-7798.

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AbstractAryl–aryl cross-coupling reactions are important reactions for the production of various biaryl compounds. This short review covers the various aryl–aryl cross-coupling reactions carried out in flow, focusing on the metal species of the aryl nucleophiles used in the cross-coupling reactions.1 Introduction2 Suzuki–Miyaura Coupling (B)3 Migita–Kosugi–Stille Coupling (Sn)4 Negishi Coupling (Zn)5 Kumada–Tamao–Corriu Coupling (Mg)6 Murahashi Coupling (Li)7 Conclusion

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38

Kansagara, N. N., V. R. Dangar, and V. R. Shah. "Synthesis, Characterization and Antimicrobial Evaluation of Schiff’s Base and Aryl Aminomethyl Derivatives." International Letters of Chemistry, Physics and Astronomy 64 (February 2016): 89–94. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.64.89.

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Schiff’s bases are obtained on heating an aldehydes with aromatic amine in presence of glacial acetic acid. These are the compounds containing characteristic –HC=N– group. Aryl amino methyl derivatives of heterocyclic compounds to synthesize by selective reduction of schiff’s bases (imine group) with sodiumborohydride in controlled experimental condition. Schiff’s base of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanimines & Aryl amines of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanamines were prepared. Their chemical structures were confirmed by means of IR, NMR, Mass data and by elemental analysis. All of the synthesized compounds were tested for their antibacterial and antifungal activity.

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Kansagara, N. N., V. R. Dangar, and V. R. Shah. "Synthesis, Characterization and Antimicrobial Evaluation of Schiff’s Base and Aryl Aminomethyl Derivatives." International Letters of Chemistry, Physics and Astronomy 64 (February 15, 2016): 89–94. http://dx.doi.org/10.56431/p-5z8xff.

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Schiff’s bases are obtained on heating an aldehydes with aromatic amine in presence of glacial acetic acid. These are the compounds containing characteristic –HC=N– group. Aryl amino methyl derivatives of heterocyclic compounds to synthesize by selective reduction of schiff’s bases (imine group) with sodiumborohydride in controlled experimental condition. Schiff’s base of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanimines & Aryl amines of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanamines were prepared. Their chemical structures were confirmed by means of IR, NMR, Mass data and by elemental analysis. All of the synthesized compounds were tested for their antibacterial and antifungal activity.

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Li, Jun, Constantin G. Daniliuc, Gerald Kehr, and Gerhard Erker. "A convenient route to internally phosphane-stabilized aryltriborane(7) compounds." Chemical Communications 54, no. 89 (2018): 12606–9. http://dx.doi.org/10.1039/c8cc06728g.

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Drapak, Iryna, Borys Zimenkovsky, Lina Perekhoda, Мargarita Suleyman, Hanna Yeromina, Natalia Skaletska, Natalya Seredynska, and Anatoly Demchenko. "Search for angiotensin II receptor antagonists among 4-aryl-n-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives." Pharmacia 66, no. 4 (December 31, 2019): 181–86. http://dx.doi.org/10.3897/pharmacia.66.e36808.

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The aim of study was to find potential antihypertensive and cardiotropic drugs among new 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imines. Materials and methods: The target compounds were synthesized by condensation asymmetrical substituted thioureas with α-bromo-4-R1-acetophenones in ethanol medium. The structure and purity of the compounds synthesized were confirmed by 1H, 13C NMR-spectroscopy and elemental analysis. Docking studies of synthesized compounds to the active site of angiotensin receptor ІІ (PDB ID: 3R8A) were performed in order to find its potential inhibitors and to select promising compounds for experimental screening. Pharmacological studies of the influence on the cardiovascular system were performed. Results: The results of docking studies indicate a high affinity of all tested substances to the selected biotarget. The thermodynamic probability of binding of synthesized substances to protein 3R8A was confirmed by negative values of scoring functions. Hydrobromide of 4-(4-methoxyphenyl)-N-phenyl-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine 3(1) and hydrobrmide of 4-(4-methoxyphenyl)-N-(4-bromphenyl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine 3(3), which have the highest negative values of scoring functions, are recommended for in vivo pharmacological studies. Based on a complete analysis of the geometric location of the synthesized compounds (ligands) in the active site of the angiotensin II receptor, it was found that the complexes are formed with the involvement of Nitrogen atom of imino group, the 1,3-thiazole ring, the phenyl and alkyl moieties of the molecule form hydrogen bonds, intermolecular electrostatic and donor-acceptor interactions. The conducted pharmacological studies of the influence on the cardiovascular system have allowed to confirm the presence of antihypertensive effect inherent in compounds of this series (except for compound 3(2)). The most effective antihypertensive effect, which is similar in duration and strength of the effect of valsartan, was the effect of compound 3(5). Conclusions: In order to expand the arsenal of biologically active substances of cardiotropic action a systematic series of new 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives were synthesized. The structure and purity of the compounds synthesized were confirmed by 1H, 13C NMR-spectroscopy and elemental analysis. Based on the results of docking studies using Autodock 4.2.6 software, selected compounds with the best affinity for protein biomes (PDB codes: 3R8A) are promising for experimental studies of hypotensive and cardiotropic activity. The most effective antihypertensive effect, which is similar in duration and strength of the effect of valsartan, was the effect of compound 3(5). A comparative analysis of the results of molecular docking and in vivo results suggests that there is a positive correlation between scoring protein inhibition and experimental data.

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Miller-Clark, Lyndsy A., Peter E. Christ, and Tong Ren. "Diruthenium aryl compounds – tuning of electrochemical responses and solubility." Dalton Transactions 51, no. 2 (2022): 580–86. http://dx.doi.org/10.1039/d1dt03957a.

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The variation of the substituents (X = 3,5-(OMe)2; 3-iPrO) on the bridging ligand results in improved solubility of Ru2-aryl compounds, while the aryl substitution significantly influences the potentials of the Ru2-based redox couples.

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Nguyen, Thanh Vinh. "A RESEARCH ON SYNTHESIS OF N-ARYL AZACYCLOALKANE UNDER MICROWAVE IRRADIATION." Journal of Science and Technique 17, no. 4 (September 27, 2022): 14–21. http://dx.doi.org/10.56651/lqdtu.jst.v17.n04.400.

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Aza-heterocyclic compounds have been known for their rich bioactivity characteristics which have been widely applied in many fields. Typically, pyrrolidine derivatives can inhibit the growth of strains of P. falciparum resistant to chloroquine. This articlepresents the research results on the synthesis of the heterocyclic compound N-aryl azacycloalkane from an alkyl halide and aniline derivatives under microwave conditions with the reaction time reduced by 20 times and the reaction efficiency doubled.

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Boyer, Jérémie, Vania Bernardes-Génisson, and Françoise Nepveu. "Access to Unsymmetrical 1,2-Diketone Intermediates via Benzeneseleninic Anhydride-Promoted Oxidation: Application to Indolone-N-Oxide Synthesis." Journal of Chemical Research 2003, no. 8 (August 2003): 507–8. http://dx.doi.org/10.3184/030823403103174731.

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1,2-Dicarbonyl compounds employed as key-intermediates in indolone-N-oxide synthesis were prepared by direct oxidation of aryl, aryl- and aryl, alkyl-substituted alkenes assisted by benzeneseleninic anhydride.

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45

Lapadatescu, Carmen, Christian Giniès, Jean-Luc Le Quéré, and Pascal Bonnarme. "Novel Scheme for Biosynthesis of Aryl Metabolites from l-Phenylalanine in the FungusBjerkandera adusta." Applied and Environmental Microbiology 66, no. 4 (April 1, 2000): 1517–22. http://dx.doi.org/10.1128/aem.66.4.1517-1522.2000.

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ABSTRACT Aryl metabolite biosynthesis was studied in the white rot fungusBjerkandera adusta cultivated in a liquid medium supplemented with l-phenylalanine. Aromatic compounds were analyzed by gas chromatography-mass spectrometry following addition of labelled precursors (14C- and 13C-labelledl-phenylalanine), which did not interfere with fungal metabolism. The major aromatic compounds identified were benzyl alcohol, benzaldehyde (bitter almond aroma), and benzoic acid. Hydroxy- and methoxybenzylic compounds (alcohols, aldehydes, and acids) were also found in fungal cultures. Intracellular enzymatic activities (phenylalanine ammonia lyase, aryl-alcohol oxidase, aryl-alcohol dehydrogenase, aryl-aldehyde dehydrogenase, lignin peroxidase) and extracellular enzymatic activities (aryl-alcohol oxidase, lignin peroxidase), as well as aromatic compounds, were detected in B. adusta cultures. Metabolite formation required de novo protein biosynthesis. Our results show that l-phenylalanine was deaminated to trans-cinnamic acid by a phenylalanine ammonia lyase and trans-cinnamic acid was in turn converted to aromatic acids (phenylpyruvic, phenylacetic, mandelic, and benzoylformic acids); benzaldehyde was a metabolic intermediate. These acids were transformed into benzaldehyde, benzyl alcohol, and benzoic acid. Our findings support the hypothesis that all of these compounds are intermediates in the biosynthetic pathway froml-phenylalanine to aryl metabolites. Additionally,trans-cinnamic acid can also be transformed via β-oxidation to benzoic acid. This was confirmed by the presence of acetophenone as a β-oxidation degradation intermediate. To our knowledge, this is the first time that a β-oxidation sequence leading to benzoic acid synthesis has been found in a white rot fungus. A novel metabolic scheme for biosynthesis of aryl metabolites froml-phenylalanine is proposed.

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46

Baranano, David, Grace Mann, and John F. Hartwig. "Nickel and Palladium-Catalyzed Cross-Couplings that Form Carbon-Heteroatom and Carbon-Element Bonds." Current Organic Chemistry 1, no. 3 (September 1997): 287–305. http://dx.doi.org/10.2174/1385272801666220124194647.

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The transition-metal catalyzed addition of heteroatom nucleophiles to aryl and vinyl halides is reviewed. This chemistry typically involves a nickel- or palladium-based catalyst containing phosphine ligands. In recently developed palladium-catalyzed chemistry, aryl halides react with amines in the presence of base to form arylamines. In similar chemistry catalyzed by both nickel and palladium, aryl and vinyl halides react with alkali metal or tin thiolates or selenides to form aryl and vinyl sulfides, while the reaction of different phosphorus compounds, such as phosphides, phosphonates, and phosphonites, with aryl halides gives compounds with new aryl-p· linkages. In addition to these typically nucleophilic heteroatoms, electrophilic heteroatoms such as boron, silicon, tin, and germanium have also been coupled to aryl electrophiles. The review closes with a brief summary of the general reaction pathways of these C-X bond-forming processes.

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Gribanov, Pavel S., Dmitry A. Loginov, Dmitry A. Lypenko, Artem V. Dmitriev, Sergey I. Pozin, Alexey E. Aleksandrov, Alexey R. Tameev, Igor L. Martynov, Andrey Yu Chernyadyev, and Sergey N. Osipov. "New Unsymmetrically Substituted Benzothiadiazole-Based Luminophores: Synthesis, Optical, Electrochemical Studies, Charge Transport, and Electroluminescent Characteristics." Molecules 26, no. 24 (December 15, 2021): 7596. http://dx.doi.org/10.3390/molecules26247596.

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Three new benzothiadiazole (BTD)-containing luminophores with different configurations of aryl linkers have been prepared via Pd-catalyzed cross-coupling Suzuki and Buchwald–Hartwig reactions. Photophysical and electroluminescent properties of the compounds were investigated to estimate their potential for optoelectronic applications. All synthesized structures have sufficiently high quantum yields in film. The BTD with aryl bridged carbazole unit demonstrated the highest electrons and holes mobility in a series. OLED with light-emitting layer (EML) based on this compound exhibited the highest brightness, as well as current and luminous efficiency. The synthesized compounds are not only luminophores with a high photoluminescence quantum yield, but also active transport centers for charge carriers in EML of OLED devices.

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Mashweu, Adelaide R., Varsha P. Chhiba-Govindjee, Moira L. Bode, and Dean Brady. "Substrate Profiling of the Cobalt Nitrile Hydratase from Rhodococcus rhodochrous ATCC BAA 870." Molecules 25, no. 1 (January 6, 2020): 238. http://dx.doi.org/10.3390/molecules25010238.

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The aromatic substrate profile of the cobalt nitrile hydratase from Rhodococcus rhodochrous ATCC BAA 870 was evaluated against a wide range of nitrile containing compounds (>60). To determine the substrate limits of this enzyme, compounds ranging in size from small (90 Da) to large (325 Da) were evaluated. Larger compounds included those with a bi-aryl axis, prepared by the Suzuki coupling reaction, Morita–Baylis–Hillman adducts, heteroatom-linked diarylpyridines prepared by Buchwald–Hartwig cross-coupling reactions and imidazo[1,2-a]pyridines prepared by the Groebke–Blackburn–Bienaymé multicomponent reaction. The enzyme active site was moderately accommodating, accepting almost all of the small aromatic nitriles, the diarylpyridines and most of the bi-aryl compounds and Morita–Baylis–Hillman products but not the Groebke–Blackburn–Bienaymé products. Nitrile conversion was influenced by steric hindrance around the cyano group, the presence of electron donating groups (e.g., methoxy) on the aromatic ring, and the overall size of the compound.

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Demchenko, Sergii, Roman Lesyk, Oleh Yadlovskyi, Johannes Zuegg, Alysha G. Elliott, Iryna Drapak, Yuliia Fedchenkova, Zinaida Suvorova, and Anatolii Demchenko. "Synthesis, Antibacterial and Antifungal Activity of New 3-Aryl-5H-pyrrolo[1,2-a]imidazole and 5H-Imidazo[1,2-a]azepine Quaternary Salts." Molecules 26, no. 14 (July 13, 2021): 4253. http://dx.doi.org/10.3390/molecules26144253.

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A series of novel 3-aryl-5H-pyrrolo[1,2-a]imidazole and 5H-imidazo[1,2-a]azepine quaternary salts were synthesized in 58–85% yields via the reaction of 3-aryl-6, 7-dihydro-5H-pyrrolo[1,2-a]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepines and various alkylating reagents. All compounds were characterized by 1H NMR, 13C NMR, and LC-MS. The conducted screening studies of the in vitro antimicrobial activity of the new quaternary salts derivatives established that 15 of the 18 newly synthesized compounds show antibacterial and antifungal activity. Synthesized 3-(3,4-dichlorohenyl)-1-[(4-phenoxyphenylcarbamoyl)-methyl]-6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-1-ium chloride 6c possessed a broad activity spectrum towards Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, and Cryptococcus neoformans, with a high hemolytic activity against human red blood cells and cytotoxicity against HEK-293. However, compound 6c is characterized by a low in vivo toxicity in mice (LD50 > 2000 mg/kg).

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Naveena Kumari, H. M., Manjunath Harihara Mathada, Mahesh Kumar, K. T. Suda, and K. M. Basavaraja. "Synthesis, Characterization, Antimicrobial Screening of 5-Bromobenzofuranyl Aryl Ureas and Carbamates." Asian Journal of Organic & Medicinal Chemistry 4, no. 4 (2019): 232–35. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p215.

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Present work reports the biologically important benzofuran aryl ureas and carbamates. The benzofuran ring was formed by reacting bromo salicylaldehyde with diethyl bromomalonate in presence of dry acetone and anhydrous potassium carbonate to obtain 5-bromo-2-ethyl carboxylate (1). The obtained ester (1) was converted into corresponding hydrazide (2) by treating with hydrazine hydrate in ethanol. Compound 2 was then converted into 5-bromobenzofuran-2-carbonyl azide (3) by treating it with sodium nitrite in dioxane and acetic acid. The compound 3 is converted into 5-bromobenzofuranyl aryl ureas (4a-e) after treating primary amines and anhydrous toluene. 5-Bromobenzofuranyl aryl carbamate (5) and ethyl carbamate (6) were also synthesized by treating compound 3 with substituted phenol in toluene and ethanol respectively. All the compounds were characterized by NMR, IR and screened for antimicrobial activities.

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Journal articles on the topic 'Aryl Compounds'

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