【摘要】 目的 设计合成一系列咪唑并[2,1-b]噻唑-5-甲酰胺类化合物，并评价其体外抗结核杆菌（MTB）活性。方法 关键中间体与母核化合物通过缩合反应制备目标物，其结构经1H-NMR、13C-NMR和MS确证。MABA法测定所有目标物及对照药对MTBH37Rv和MDR-MTB的MIC值。结果 合成了30个咪唑并[2,1-b]噻唑-5-甲酰胺类化合物（包括先导物A）。部分目标物对两株MTB均敏感（MIC<0.016～0.211μg/ml），其中1e的体外活性与Q203相当，而优于先导物A。结论 丰富了咪唑并[2,1-b]噻唑-5-甲酰胺类化合物抗结核构效关系，为下一步相关研究奠定了基础。更多还原

【Abstract】 Objective We aim to design and synthesize a series of new imidazo[2,1-b]thiazole-5-carboxamides, and evaluate their in vitro antitubercular activity.Methods Target compounds were synthesized through condensation of key intermediates with imidazo[2,1-b]thiazole-5-carboxamide cores. Their structures were characterized by 1H-NMR, 13C-NMR and MS. In vitro antitubercular activity of the compounds were evaluated by MABA assay.Results Thirty compounds including the lead compound A were synthesized in this study. Some of them were found to be active against both the two MTB strains(MIC < 0.016-0.211 μg/ml), and compound 1 e was more active than the lead compound A and comparable to Q203. Conclusion This study enriches the structure activity relationship information of imidazo[2,1-b]thiazole-5-carboxamides against MTB, which lays the foundation for the future research.更多还原