Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin

被引：43

作者：

Bhattacharya, G ^{[1
]}

Salem, MM ^{[1
]}

Werbovetz, KA ^{[1
]}

机构：

[1] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00465-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel dinitroaniline sulfonamides based on the herbicide oryzalin 3 were synthesized and evaluated for activity against the parasitic protozoan Leishmania donovani and against leishmanial tubulin, the putative antiparasitic target of oryzalin. A subset of these compounds possess more activity against both Leishmania and the target protein in vitro. Compound 20 displays improved potency against leishmanial tubulin and is 13.4-fold more active against L. donovani axenic amastigotes than oryzalin. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2395 / 2398

页数：4

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