Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines
Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines
复制标题
DOI：
10.1093/jac/dki319
复制
发表时间：
2005-11-01
影响因子：
5.2
通讯作者：
Nacy, CA
中科院分区：
文献类型：
--
作者：
Protopopova, M;Hanrahan, C;Nacy, CA
目的：本研究的目的是确定一个候选药物的临床开发，从以前合成的组合库的基础上的1，2-乙二胺结构的ethambutol.Methods：六十九个最有效的打击对结核分枝杆菌的原始研究进行了一系列的测试，在体外和体内测定的MIC为M。结果：27个化合物的MIC为1.05，
Objectives: The aim of this study was to identify a candidate drug for clinical development from a previously synthesized combinatorial library based on the 1,2-ethylenediamine structure of ethambutol.Methods: Sixty-nine of the most potent hits against Mycobacterium tuberculosis from the original studies were subjected to a sequential set of tests in vitro and in vivo-determination of MIC for M. tuberculosis H37Rv, cytotoxicity, intracellular antimycobacterial activity, permeability evaluation and in vivo efficacy testing.Results: Twenty-seven compounds with MICs of