Synthesis and biological evaluation of indolyl glyoxylamides as a new class of antileishmanial agents

被引:19
作者
Chauhan, Shikha S. [1 ]
Gupta, Leena [1 ]
Mittal, Monika [2 ]
Vishwakarma, Preeti [2 ]
Gupta, Suman [2 ]
Chauhan, Prem M. S. [1 ]
机构
[1] CSIR, Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
关键词
Antileishmanial; Indolylglyoxylamides; Tetrahydro-beta-carboline; TETRAHYDRO-BETA-CARBOLINES; ACTIVE ANTICANCER AGENTS; ALKALOIDS; LEISHMANIASIS; ANALOGS;
D O I
10.1016/j.bmcl.2010.08.119
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of indolylglyoxylamide derivatives have been synthesized and evaluated in vitro against amastigote form of Leishmania donovani. Compound 8c has been identified as the most active analog of the series with IC(50) value of 5.17 mu M and SI value of 31.48, and is several folds more potent than the standard drugs sodium stilbogluconate and pentamidine. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6191 / 6194
页数:4
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