Structure-activity relationships in 2-aminodiphenylsulfides against trypanothione reductase from Trypanosoma cruzi

被引：24
|
作者：
Girault, S
Davioud-Charvet, E
Salmon, L
Berecibar, A
Debreu, MA
Sergheraert, C
机构：
[1] Fac Pharm, Inst Biol, F-59021 Lille, France
[2] Fac Pharm, Inst Pasteur, CNRS, URA 1309, F-59021 Lille, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 10期
关键词：
D O I：
10.1016/S0960-894X(98)00180-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In order to establish structural elements responsible for inhibition of trypanothione reductase (TR) from Trypanosoma cruzi by 2-aminodiphenylsulfides, a series of dissymmetrical derivatives, corresponding to the replacement of one aromatic moiety by different amines, was synthesized. TR inhibition studies revealed the importance of the aromatic rings and of the amino groups in the side chains for potent inhibition. Quinonic moities were also introduced with the aim of acting as TR redox-cycling substrates. (C) 1998 Elsevier Science Ltd. All rights reserved.
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收藏
页码：1175 / 1180
页数：6
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