各种取代的1,8-萘啶衍生物的合成及其抗分枝杆菌活性评估。

Synthesis of variously substituted 1,8-naphthyridine derivatives and evaluation of their antimycobacterial activity.

作者信息

Badawneh Muwaffag, Manera Clementina, Mori Claudio, Saccomanni Giuseppe, Ferrarini Pier Luigi

机构信息

Philadelphia University, Sweileh, Jordan.

出版信息

Farmaco. 2002 Aug;57(8):631-9. doi: 10.1016/s0014-827x(02)01235-1.

DOI:10.1016/s0014-827x(02)01235-1

PMID:12361230

Abstract

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 tuberculosis H37Rv, showed an interesting activity with % inhibition in the range 38-96%. The most effective substituent in position 2, 4 or 7 of the 1,8-naphthyridine nucleus seem to be the piperidinyl group.

摘要

根据与结核病抗菌药物采购与协调机构（TAACF）合作的一项国际计划，合成了一系列在2、3、4和7位有不同取代基的1,8-萘啶衍生物，用于体外抗分枝杆菌活性评估。几种化合物4、8、12、14、19、29和30，当以6.25微克/毫升的浓度对结核分枝杆菌H37Rv进行测试时，显示出有趣的活性，抑制率在38%-96%之间。1,8-萘啶核2、4或7位最有效的取代基似乎是哌啶基。