Abstract

A new series of maleimide triazole hybrid compounds namely 3-chloro-1-[(1-aryl-1H-1,2,3-triazol-4-yl)methyl]-4-(arylamino)-1H-pyrrole-2,5-dione have been prepared. Our synthetic strategy starts via the reaction of 2,3-dichloromaleic anhydride with propargyl amine followed by chlorine displacement with arylamine and subsequent formation of a triazole utilizing copper(I) catalyzed azide-alkyne cycloaddition reaction, that generates the designed triazole nucleus. The produced hybrid compounds were identified using various physicochemical properties of the pure compounds. The synthesized compounds were screened for antimicrobial activities against Escherichia coli, Pseudomonas aeruginosa, and Bacillus spizizenii. While selected compounds were tested for their anticancer activities against T47D, HCT 116, and VERO cell lines.

Graphic abstract

中文翻译：

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新型马来酰亚胺1,2,3-三唑杂化物：设计，合成，抗癌和抗菌活性

摘要

一系列新的马来酰亚胺三唑杂化化合物，即3-氯-1-[（1-芳基-1 H -1,2,3-三唑4-基）甲基] -4-（芳基氨基）-1 H-吡咯-已经制备了2，5-二酮。我们的合成策略开始于2,3-二氯马来酸酐与炔丙基胺的反应，接着是氯与芳基胺的置换，以及随后利用铜（I）催化的叠氮化物-炔烃环加成反应形成三唑，从而生成设计的三唑核。使用纯化合物的各种理化特性鉴定了产生的杂化化合物。筛选合成的化合物对大肠杆菌，铜绿假单胞菌和spizizenii的抗菌活性。同时测试了所选化合物对T47D，HCT 116和VERO细胞系的抗癌活性。

图形摘要