目的:本研究旨在通过将生物活性杂合药效团(噻唑环和咪唑并[2,1-b]噻唑系统)整合到一个生物评估分子系统中来合成它们。
背景:文献调查显示,各种咪唑并[2,1-b]噻唑,噻唑,和腙具有强大的抗分枝杆菌活性。
目的:这项研究证明了分子杂交的有效性以及咪唑并[2,1-b]噻唑-腙-噻唑作为有前途的抗分枝杆菌药物的开发范围。
方法:几种咪唑并[2,1-b]噻唑-肼-噻唑5a-g,7a,B,9a,B,11a,B,13和15a,使用分子杂交策略产生b,并针对结核分枝杆菌(ATCC25618)评估其体外抗结核活性。
结果:衍生物7b(MIC=0.98μg/mL)在测试的系列中显示出最有希望的抗分枝杆菌活性。简要的构效关系研究发现,对氯苯或吡啶的噻唑,或香豆素与抗微生物杆菌活性有显著关系。
结论:与参考药物相比,化合物7b的抗分枝杆菌活性有希望,这表明该化合物可能作为寻找新的潜在抗分枝杆菌药物的先导化合物。
OBJECTIVE: 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.
BACKGROUND: A literature survey revealed that various imidazo[2,1-b]thiazoles, thiazoles, and hydrazones have powerful antimycobacterial activity.
OBJECTIVE: 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.
METHODS: 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.
RESULTS: 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.
CONCLUSIONS: 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.