Trypanothione reductase inhibition/trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series

被引：53
作者：
Bonnet, B
Soullez, D
Girault, S
Maes, L
Landry, V
Davioud-Charvet, E
Sergheraert, C
机构：
[1] Univ Lille 2, Fac Pharm, Inst Biol, F-59021 Lille, France
[2] Univ Lille 2, Fac Pharm, Inst Pasteur Lille, CNRS,UMR 8525, F-59021 Lille, France
[3] Janssen Res Fdn, B-2340 Beerse, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2000年 / 8卷 / 01期
关键词：
chemotherapy; antiparasitics; enzyme inhibitors; polycyclic heterocyclic compounds;
D O I：
10.1016/S0968-0896(99)00268-0
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：
A series of symmetrically substituted 1,4-bis(3-aminopropyl)piperazines was synthesized and tested towards trypanothione reductase and for its in vitro trypanocidal potency. The most trypanocidal amongst them was found to be totally inactive towards the enzyme and thus constitutes a lead structure for the identification of new potential Trypanosoma cruzi target(s). (C) 2000 Elsevier Science Ltd. All rights reserved.
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收藏
页码：95 / 103
页数：9
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