جستجوی مقالات مرتبط با کلیدواژه « thiazolidinone » در نشریات گروه « شیمی »

In this study, synthesis of novel Mannich bases, Schiff bases, and heterocyclic compounds starting from quinoline-2-carboxylic acid has been achieved and their antimicrobial activities were studied. The first step involved the synthesis of compound E1 from reaction of 2-quinolinyl chloride with hydrazine. In the second step, compound E2 was prepared from the reaction of E1 with CS2 in an alkaline medium. The third step included the preparation of compounds E3-E7 from the reaction of E2 with different amines. In the fourth step, compound E8 was synthesized from the reaction of compound E2 with ethyl-2-chloroacetate in the presence of potassium carbonate. In the fifth step, compound E9 was prepared from the reaction of compound E8 with hydrazine in absolute ethanol. In the sixth step, compounds E10-E12 were prepared from a condensing reaction between compound E9 and different aromatic aldehydes. In the seventh step, compounds E13-E18 were prepared, respectively, from the reaction of thioglycolic acid and sodium azide with compounds E10-E12. Finally, the prepared compounds were characterized by FT-IR and 1H-NMR spectroscopy, and their antimicrobial activities were studied.

In this work, a novel series of mefenamic acid analogs were developed and synthesized with the goal of developing a lead chemical that has anti-inflammatory efficacy and avoids the adverse effects of NSAIDs. Molecular docking analysis was performed by recruiting the ligands, COX-1 and COX-2 to identify the best-fitted molecule using AutoDock software. Afterwards, the compounds were synthesized and analyzed. To assess the drug's efficacy, the compounds were subjected to in vivo analgesic and anti-inflammatory experiments. Most of synthesized ligands have greater binding free energy than mefenamic acid on COX-1. When compared to the positive control, the compounds 2-(2,3-dimethylphenylamino)-N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-4-oxothiazolidin-3-yl) benzamide, 2-(2,3-dimethylphenylamino)-N-(2-(4-fluorophenyl)-4-oxothiazolidin-3-yl)benzamide, 2-(2, 3-dimethylphenylamino)-N-(4-oxo-2-p-tolylthiazolidin-3-yl) benzamide and 2-(2,3-dimethylphenylamino)-N-(2-(4-chlorophenyl)-4-oxothiazolidin-3-yl) benzamide, 2-(2,3-dimethylphenylamino)-N-(2-(4-nitrophenyl)-4-oxothiazolidin-3-yl)benzamide demonstrated a larger or comparable proportion of analgesic and anti-inflammatory action respectively. Furthermore, the selected compounds “2-(2,3-dimethylphenylamino)-N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-4-oxothiazolidin-3-yl) benzamide”, and “2-(2,3-dimethylphenylamino)-N-(4-oxo-2-p-tolylthiazolidin-3-yl) benzamide” seemed to have the least ulcerogenic activity. These findings show that some of the newly created mefenamic acid analogs may be selected as lead compounds due to their significant biological properties without ulcerogenic activity.

In this work, 2-amino pyridine was mixed with biphenyl bromide under refluxed to give the product of 2-biphenyl imidazo [1,2-a] pyridine (1). Compound (1) was treated with 4-amino acetophenone with formaldehyde dissolved in absolute ethanol to yield Mannich base (2). Schiff bases [3I-3K] were also prepared by condensed compound (2) dissolved in absolute ethanol with few drops of glacial acetic acid and different aromatic amines. After that, Schiff bases were cyclized using three reagents such as marcapto acetic acid, succinic anhydride, and 3-Nitrophthalic anhydride dissolved in absolute ethanol under refluxed at certain temperature to form thiozolidinone (4I-4K), (1,3)oxazepine-4,7-dione (5K-5I) and 4-Nitro benzo (1,3) oxazepine-4,7-dione (6I-6K) compounds. All compounds were characterized by FT-IR, 1H-NMR, and 13C-NMR spectra. Some new compounds were evaluated as antioxidant and anticorrosion agents.

The present study includes the synthesis and characterization of thiazolidinedion containing indole ring. Two compounds were prepared: (4-fluorophenyl)-2-(1H-indol-3-yl)thiazolidin-4-one (I) and(4-( dimethylamino)phenyl)-2-(1H-indol-3-yl)thiazolidin-4-one(II), the prepared compounds  diagnosed by using infrared spectra, NMR spectra (1H-NMR), and the results were identical to what is expected in practice. The Gaussian program was used for the computational study of thiazolidinedion and the theoretical calculations of the thermodynamic variables showed that compound (I) is the more softness with the lowest hardness. Meanwhile, compound (II) the more hardness with less softness.

Several new 2-pyridyl-4-thiazolidinones are synthesized in an efficient manner evading using any catalyst or base. Simple workup procedure, good yields, and mild reaction conditions are the salient features of this method. All the synthesized compounds are screened for antimicrobial activity against several organisms.

A series of novel 1, 8-dioxo-octahydroxanthene derivatives containing 4-thiazolidinone framework (4a-f) were synthesized through a four-step reaction starting from the reduction of nitro derivatives of 1, 8-dioxo-octahydroxanthenes. The resulting aminoxanthenes converted to thiourea derivatives via their reaction with methyl isothiocyanate. The final products were synthesized through the reaction of thiourea derivatives with dialkylacetylene dicarboxylates. All of the steps were carried out under easy and mild reaction conditions in the absence of expensive catalysts or esoteric starting materials. The structures of compounds 3a-c and the final products were characterized according to their physical constants, spectral data such as NMR, IR spectra and also elemental analysis.

Utilization of benzoxazinone for synthesis quinazolinone derivatives with 3-heterocycle side chain. treatment of benzoxazinon 1 with cyano acetohydrazide or thionocarbohydrazide gave the quinazolinone derivatives 2 or 12. quinazolinone 2 has been utilized as synthon for new  pyridinone, oxazet, thiazole, thiazolidinone and quinazolinone derivatives. Thiosemicarbazide and thiosemicarbazone derivatives are synthesized from quinazolinone 12 by different route. The structures of the new compounds were established on the basis of IR, 1HNMR, mass spectral data, and elemental analysis.