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

被引：17
|
作者：
Wiesner, J
Mitsch, A
Wissner, P
Krämer, O
Jomaa, H
Schlitzer, M
机构：
[1] Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
[2] Univ Klin Giessen, Inst Biochem, D-35249 Giessen, Germany
[3] Jomaa Pharmaka GmbH, D-35249 Giessen, Germany
[4] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 19期
关键词：
D O I：
10.1016/S0960-894X(02)00555-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In a previous report, we have described novel anti-malarial compounds based on a 2,5-diaminobenzophenone scaffold. Here, we have invesigated acryloyl derivatives carrying a biaryl structure consisting of a terminal aryl residue and a central 2-furyl ring. Several compounds were obtained in the series of para-substituted phenylfurylacryloyl derivatives that displayed improved anti-malarial activity in comparison to earlier described derivatives. From the structure-activity relationships it can be deduced that there has to be a lipophilic moiety in the para-position of the terminal phenyl residue. Furthermore, there are indications that, alternatively, activity may benefit from the presence of a polar moiety with hydrogen bond acceptor properties. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2681 / 2683
页数：3
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