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Synthesis of Novel Quinoline–Benzoxazolinone Ester Hybrids: In Vitro Anti-Inflammatory Activity and Antibacterial Activity
Russian Journal of Bioorganic Chemistry ( IF 1 ) Pub Date : 2021-04-26 , DOI: 10.1134/s1068162021020242
Sarfaraz F. Shaikh , Pratik P. Dhavan , Pinky R. Singh , S. P. Vaidya , B. L. Jadhav , M. M. V. Ramana

Abstract

A series of novel quinoline-benzoxazolinone ester hybrids were synthesized characterized and assessed for their in vitro anti-inflammatory and antibacterial activity. The in vitro anti-inflammatory activity was executed using protein denaturation assay, proteinase inhibitory assay and human red blood cell membrane stabilization assay. Most of the compounds exhibited potential anti-inflammatory activity. Compound (2-oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(thiophen-2-yl)quinoline-4-carboxylate showed a better anti-inflammatory activity than the standard drugs diclofenac sodium and indomethacin. Furthermore, antibacterial activities of the synthesized compounds were evaluated using resazurin microtiter assay (REMA) and were compared with a positive drug standard chloramphenicol. The compounds demonstrated moderate to potent antibacterial activity. (2-Oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(3,4-dimethoxyphenyl)quinoline-4-carboxylate and (2-oxobenzo[d]oxazol-3(2H)-yl)methyl-2-(2-chlorophenyl)quinoline-4-carboxylate displayed excellent activity against all bacterial strains in comparison to standard chloramphenicol. Moreover, cytotoxicity was performed on MDCK cells using MTT assay and it was found that none of the synthesized derivatives possessed any cytotoxicity.



中文翻译:

新型喹啉-苯并恶唑啉酮酯杂化物的合成:体外抗炎活性和抗菌活性

摘要

合成了一系列新颖的喹啉-苯并恶唑啉酮酯杂化物,表征并评估了它们的体外抗炎和抗菌活性。使用蛋白质变性测定,蛋白酶抑制测定和人红细胞膜稳定测定执行体外抗炎活性。大多数化合物表现出潜在的抗炎活性。化合物(2-氧代苯并[ d ]恶唑-3(2 H)-基)甲基-2-(噻吩-2-基)喹啉-4-羧酸盐显示出比标准药物双氯芬酸钠和消炎痛更好的抗炎活性。此外,使用刃天青微量滴定法(REMA)评估了合成化合物的抗菌活性,并将其与阳性药物标准氯霉素进行了比较。该化合物显示出中等至有效的抗菌活性。(2-氧代苯并[ d ]恶唑-3(2 H)-基)甲基-2-(3,4-二甲氧基苯基)喹啉-4-羧酸酯和(2-氧代苯并[ d ]恶唑-3(2 H)-基)甲基-2-(2-氯苯基)喹啉-4-羧酸酯与标准氯霉素相比,对所有细菌菌株均显示出优异的活性。此外,使用MTT测定法对MDCK细胞进行了细胞毒性,发现合成的衍生物均不具有任何细胞毒性。

更新日期:2021-04-27
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