抗细菌
噻唑
化学
组合化学
立体化学
结核分枝杆菌
肺结核
医学
病理
作者
Huda K. Mahmoud,Abdelwahed R. Sayed,Marwa M. Abdel‐Aziz,Sobhi M. Gomha
出处
期刊:Medicinal Chemistry
日期:2022-04-15
卷期号:18 (10): 1100-1108
被引量:10
标识
DOI:10.2174/1573406418666220413095854
摘要
The study aims to synthesize bioactive hybrid pharmacophores (thiazole ring and imidazo[2,1-b]thiazole system) by incorporating them into one biological assessment molecular system.A literature survey revealed that various imidazo[2,1-b]thiazoles, thiazoles, and hydrazones have powerful antimycobacterial activity.This study demonstrates the effectiveness of molecular hybridization and the scope for imidazo[2,1-b]thiazole-hydrazone-thiazoles to develop as promising antimycobacterial agents.Several imidazo[2,1-b]thiazole-hydrazine-thiazoles 5a-g, 7a,b, 9a,b, 11a,b, 13, and 15a,b were generated using a molecular hybridization strategy and assessed against Mycobacterium tuberculosis (ATCC 25618) for their in vitro antituberculous activity.Derivative 7b (MIC = 0.98 μg/mL) has shown the most promising antimycobacterial activity among the series tested. Brief structure-activity relationship studies found that the thiazole of chlorophenyl or pyridine, or coumarin had a significant relation with the antimycobacterial activity.The promising antimycobacterial activity of compound 7b compared with the reference drug suggests that this compound may contribute as a lead compound in the search for new potential antimycobacterial agents.
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