Design and synthesis of new antimalarial agents from 4-aminoquinoline

被引:74
作者
Solomon, VR
Puri, SK
Srivastava, K
Katti, SB [1 ]
机构
[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
关键词
4-aminoquinoline; antimalarial; heam binding;
D O I
10.1016/j.bmc.2004.12.051
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
This study describes the synthesis of new 4-aminoquinoline derivatives and evaluation of their activity against a chloroquine sensitive strain of P. falciparum in vitro and chloroquine resistant N-67 strain of P. yoelii in vivo. All the analogues were found to form strong complex with hematin and inhibit the P-hematin formation in vitro. These results suggest that these compounds act on heme polymerization target. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2157 / 2165
页数:9
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