Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine

被引：102

作者：

Chibale, K ^{[1
]}

Haupt, H

Kendrick, H

Yardley, V

Saravanamuthu, A

Fairlamb, AH

Croft, SL

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

[2] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Med, London WC1E 7HT, England

[3] Univ Dundee, Wellcome Trust Bioctr, Sch Life Sci, Div Biol Chem & Mol Microbiol, Dundee DD1 5EH, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 19期

基金：

英国惠康基金; 新加坡国家研究基金会;

关键词：

D O I：

10.1016/S0960-894X(01)00528-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Sulfonamide and urea derivatives of quinacrine with varying methylene spacer lengths were synthesised and tested for inhibition of trypanothione reductase (TryR) and for activity in vitro against strains of the parasitic protozoa Trypanosoma, Leishmania, and Plasmodium. These derivatives are superior inhibitors of TryR relative to quinacrine with the best compound being 40 times more potent. Urea derivatives generally displayed good in vitro activity against all parasites. (C) 2001 Elsevier Science Ltd. All rights reserved.

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收藏

页码：2655 / 2657

页数：3

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