Structure-activity relationships of novel anti-malarial agents.: Part 3:: N-(4-acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides

被引：32
|
作者：
Wiesner, J
Kettler, K
Jomaa, H
Schlitzer, M
机构：
[1] Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany
[2] Univ Giessen Klinikum, Biochem Inst, D-35249 Giessen, Germany
[3] Jomaa Pharm GmbH, D-35249 Giessen, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期
关键词：
D O I：
10.1016/S0960-894X(01)00798-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We have described 5-(4-propoxycinnamoylamino)-2-(4-tolylacetylamino)benzophenone 6e as a novel lead for antimalarial agents. Anti-malarial activity of these 5-(4-propoxycinnamoylamino)benzophenones proved to be quite sensitive against variations of the acyl substituent at the 2-amino group. Best activity was obtained with phenylacetic acid moieties carrying small substituents in the para-position. From the para-substituents evaluated, the trifluoromethyl group yielded the most active compound (6j) in this series (IC50 = 120 nM). Deviations from the phenylacetic acid substructure, shifting the substituent into the ortho-position or bulkier para-substituents resulted in a significant reduction in anti-malarial activity. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：543 / 545
页数：3
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