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Design and synthesis of novel isatin derivatives as potent analgesic, anti-inflammatory and antimicrobial agents
Journal of Chemical Sciences ( IF 1.7 ) Pub Date : 2020-08-04 , DOI: 10.1007/s12039-020-01795-0
Kosaraju Lahari , Raja Sundararajan

Abstract

A powerful analgesic, anti-inflammatory and antimicrobial drug was developed by synthesizing a set of new indole-2,3-dione derivatives. The chemical structures of the synthesized derivatives were confirmed by spectroscopic and elemental analyses. Tail flick method, carrageenan-induced foot paw edema technique and agar streak dilution methods were employed to evaluate analgesic, anti-inflammatory and antimicrobial activities (in vitro) of drugs, respectively. In addition, ulcerogenicity of potent derivatives was also estimated. Most of the synthesized derivatives displayed low-to-reasonable ulcer index, with mild-to-good analgesic, anti-inflammatory and antimicrobial potency. The SARs between the biological activity and differences in the functional group of the title compounds have been explained. 1-(4-Chlorobenzylidene)-4-(4-(1-((dimethylamino)methyl)-5-nitro-2-oxoindolin-3-ylideneamino)phenyl)thiosemicarbazide VIc has been found as the potent derivative of this series.

Graphic abstract

A set of new indole-2,3-dione derivatives was synthesized from isatin and tested for analgesic, anti-inflammatory and antimicrobial activities. Furthermore, ulcerogenicity of potent derivatives was also estimated. The SARs between biological activity and differences in functional groups of the test derivatives are explained.


中文翻译:

作为有效的止痛,消炎和抗菌剂的新型伊斯汀衍生物的设计和合成

摘要

通过合成一组新的吲哚-2,3-二酮衍生物,开发了一种功能强大的止痛,抗炎和抗菌药物。通过光谱和元素分析证实了合成衍生物的化学结构。甩尾法,角叉菜胶诱发的足爪浮肿技术和琼脂条纹稀释法用于评估镇痛,抗炎和抗菌活性(体外)的药物。另外,还估计了有效衍生物的致溃疡性。大多数合成衍生物显示出低至合理的溃疡指数,具有轻至良好的止痛,抗炎和抗菌功效。已经说明了生物学活性与标题化合物官能团差异之间的SAR。已发现1-(4-氯亚苄基)-4-(4-(1-(((二甲基氨基)甲基)-5-硝基-2-氧吲哚-3-基亚氨基氨基)苯基)硫代氨基脲VIc是该系列的有效衍生物。

图形摘要

从靛红合成了一组新的吲哚-2,3-二酮衍生物,并测试了其镇痛,抗炎和抗菌活性。此外,还估计了有效衍生物的致溃疡性。解释了生物活性和测试衍生物的官能团差异之间的SAR。
更新日期:2020-08-04
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