Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, China.
Eur J Med Chem. 2012 Mar;49:164-71. doi: 10.1016/j.ejmech.2012.01.007. Epub 2012 Jan 12.
A series of substituted 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives were synthesized. The derivatives were screened for in vitro anti-tubercular activities against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA), and antibacterial activities with agar dilution method against clinical S. aureus, E. coli, S. pneumoniae and penicilin-resistant S. pneumoniae. Among 15 compounds, several thiazole derivatives exhibited good anti-tubercular activities with MIC values between 1 μM and 61.2 μM, and potent activities against S. pneumoniae with MIC values less than 0.134 μM. These studies suggest that the thiazole scaffold may serve as a new promising template for further elaboration as anti-tubercular and antibacterial drugs.
一系列取代的 4-(2,6-二氯苄氧基)苯基噻唑、噁唑和咪唑衍生物被合成。使用微孔板 Alamar 蓝检测法（MABA），这些衍生物被筛选出对结核分枝杆菌 H37Rv 的体外抗结核活性，并用琼脂稀释法对临床金黄色葡萄球菌、大肠杆菌、肺炎链球菌和青霉素耐药肺炎链球菌进行抗菌活性检测。在 15 种化合物中，几种噻唑衍生物表现出良好的抗结核活性，MIC 值在 1 μM 至 61.2 μM 之间，对肺炎链球菌具有强大的活性，MIC 值小于 0.134 μM。这些研究表明，噻唑支架可以作为进一步开发抗结核和抗菌药物的新的有前途的模板。
