作者:Aldo Andreani、Massimiliano Granaiola、Alberto Leoni、Alessandra Locatelli、Rita Morigi、Mirella Rambaldi
DOI:10.1016/s0223-5234(01)01266-1
日期:2001.9
selected imidazo[2,1-b]thiazoles entered the screening at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) and one of these compounds, 2-chloro-6-phenylimidazo[2,1-b]thiazole, showed antitubercular activity. On this basis we planned the synthesis of new analogues bearing a substituted ring at the 6 position. For one compound only (2-chloro-6-p-chlorophenylimidazo[2,1-b]thiazole)
许多选定的咪唑并[2,1-b]噻唑在结核病抗菌素获取和协调机构(TAACF)处进行了筛选,其中一种化合物2-氯-6-苯基咪唑并[2,1-b]噻唑显示抗结核活性。在此基础上,我们计划合成在6位带有取代环的新类似物。仅对于一种化合物(2-氯-6-对氯苯基咪唑并[2,1-b]噻唑),还制备了5-亚硝基衍生物。将这些化合物的抗结核活性与已知的在2位上缺少氯的类似物进行了比较。5-亚硝基-6-对氯苯基咪唑并[2,1-b]噻唑表现出有效的抗结核活性。