碳酰胺衍生物的硅、抗菌和细胞毒性研究及其绿色合成

Q4 Pharmacology, Toxicology and Pharmaceutics

INDIAN DRUGS Pub Date : 2023-10-28 DOI:10.53879/id.60.10.14103

Swathi Thumula, Venkatesan Srinivasadesikan, Ravi K. Kottalanka, Ramu Samineni

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引用次数: 0

摘要

以2-(氧基-2-甲基)异吲哚- 1,3 -二酮、4-(4-氨基苯基)morpholin-3- 1和5-氯噻吩-2-羰基氯为原料，采用分步合成法合成了5-氯- n-((2-氧基-3-(4-(3-氧基)苯基)恶唑烷-5-基)甲基)噻吩-2-羧酰胺衍生物。设计、制备并筛选了3个化合物3、4、7对HeLa、MCF- 7、A-549、K-562的抑癌活性以及对Gram +ve和Gram -ve的抑菌活性。羧胺部分被证明能够开发新的抗癌和抗菌药物。靶向受体caspase-3 HeLa细胞系与金黄色葡萄球菌DNA-Gyrase的对接研究也支持化合物3、4和7的抗癌和抗菌活性

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IN SILICO, ANTIMICROBIAL AND CYTOTOXIC STUDIES OF CARBOXAMIDE DERIVATIVES AND THEIR GREEN SYNTHESIS

5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino) phenyl) oxazolidin-5-yl) methyl) thiophene-2-carboxamide derivatives were synthesized in a simple and efficient approach using 2-(oxiran-2-ylmethyl) isoindoline-1, 3-dione, 4-(4-aminophenyl) morpholin-3-one, and 5-chlorothiophene-2-carbonyl chloride by stepwise synthesis. Three compounds 3, 4 and 7 were designed, prepared, and screened for anticancer activity against HeLa, MCF- 7, A-549 and K-562 and antibacterial activities against Gram +ve and Gram -ve strains. The carboxamide moieties proved to be capable for the development of new anticancer and anti-bacterial agents. Docking studies carried out on target receptors caspase-3 HeLa cell line and Staphylococcus aureus DNA-Gyrase also supported the anticancer and antimicrobial activity of compounds 3, 4 and 7

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来源期刊

INDIAN DRUGS Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

0.30

自引率

0.00%

发文量