Structure-activity relationships of novel anti-malarial agents.: Part 7:: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-uryl)acrylic acid amides with polar moieties

被引：21
|
作者：
Wiesner, J
Mitsch, A
Jomaa, H
Schlitzer, M
机构：
[1] Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
[2] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany
[3] Univ Giessen, Inst Biochem, D-35249 Giessen, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 13期
关键词：
D O I：
10.1016/S0960-894X(03)00353-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In a previous report, we have provided evidence that novel anti-malarial compounds based on 2,5-diaminobenzophenone farnesyltransferase inhibitors might benefit from the presence of a polar moiety at the para position of the terminal phenyl of the arylfurylacryloyl partial structure. Here, we demonstrate that different moieties with hydrogen bond acceptor properties lead to equipotent or even improved anti-malarial activity in comparison to the nitro group described before. (C) 2003 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2159 / 2161
页数：3
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