Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

被引:108
作者
Madrid, PB
Sherrill, J
Liou, AP
Weisman, JL
DeRisi, JL
Guy, RK [1 ]
机构
[1] Univ Calif San Francisco, Dept Pharmaceut Chem, San Francisco, CA 94143 USA
[2] Univ Calif San Francisco, Dept Biochem & Biophys, San Francisco, CA 94143 USA
[3] Univ Calif San Francisco, Dept Cellular & Mol Pharmacol, San Francisco, CA 94143 USA
关键词
D O I
10.1016/j.bmcl.2004.12.037
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1015 / 1018
页数:4
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