Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts

被引：70

作者：

Musonda, CC

Taylor, D

Lehman, J

Gut, J

Rosenthal, PJ

Chibale, K ^{[1
]}

机构：

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

[2] Univ Cape Town, Sch Med, Div Pharmacol, Dept Med,Observ, ZA-7925 Cape Town, South Africa

[3] Univ Calif San Francisco, Dept Med, San Francisco, CA 94143 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期

基金：

新加坡国家研究基金会;

关键词：

Ugi isocyanide multi-component reactions; malaria; 4-aminoquinolines;

D O I：

10.1016/j.bmcl.2004.05.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a new class of Ugi adducts incorporating the 4-aminoquinoline moiety is described. The novel compounds are active against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with the best compound showing an IC50 value of 73 nM against a resistant K1 strain. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：3901 / 3905

页数：5

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