Synthesis of variously substituted 1,8-naphthyridine derivatives and evaluation of their antimycobacterial activity
作者:Muwaffag Badawneh、Clementina Manera、Claudio Mori、Giuseppe Saccomanni、Pier Luigi Ferrarini
DOI:10.1016/s0014-827x(02)01235-1
日期:2002.7
A series of 1,8-naphthyridine derivatives variously substituted in the 2, 3, 4 and 7 positions were synthesized for in vitro evaluation of antimycobacterial activity in accordance with an international program with the tuberculosis antimicrobial acquisition and coordinating facility (TAACF). Several compounds 4, 8, 12, 14, 19, 29 and 30, when tested at a concentration of 6.25 microg/ml against Mycobacterium
合成了一系列分别在2、3、4和7位取代的1,8-萘啶衍生物,用于根据国际计划与结核病抗微生物药物获取和协调设施(TAACF)进行体外评估,以评估抗分枝杆菌的活性。当以6.25微克/毫升的浓度针对结核分枝杆菌H37Rv进行测试时,几种化合物4、8、12、14、19、29和30表现出令人感兴趣的活性,%抑制率在38-96%的范围内。1,8-萘啶核的2、4或7位上最有效的取代基似乎是哌啶基。