Synthesis of indolizine derivatives with selective antibacterial activity against Mycobacterium tuberculosis
作者:Lise-Lotte Gundersen、Colin Charnock、Ayele Hailu Negussie、Frode Rise、Solomon Teklu
DOI:10.1016/j.ejps.2006.09.006
日期:2007.1
1-substituted indolizines with activity against Mycobacterium tuberculosis have been synthesized. The most active compounds carry an hydroxyphenylmethyl- or hydroxyalkyl substituent in the indolizine 1-position. The alkyl chain should be moderately long (C-5 or C-6). Aryl groups in the 2- and 3-position of the indolizine are also required. Removal of the 3-substituent resulted in significant loss of
已经合成了具有抗结核分枝杆菌活性的1-取代的吲哚嗪。最具活性的化合物在吲哚嗪1位上带有羟苯基甲基或羟烷基取代基。烷基链应适当长(C-5或C-6)。还需要吲哚嗪的2-和3-位的芳基。除去3-取代基导致活性显着丧失。7位的腈取代基对化学稳定性和生物活性均有利。化合物研究显示窄的抗菌谱,并且似乎是相当选择性抗分支杆菌的化合物。还观察到针对某些病原虫的中等活性。