Structure-activity relationships of novel anti-malarial agents:: Part 5.: N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides

被引：19

作者：

Wiesner, J

Kettler, K

Sakowski, J

Ortmann, R

Jomaa, H

Schlitzer, M

机构：

[1] Univ Munich, Zentrum Pharmaforsch, Dept Pharm, D-81377 Munich, Germany

[2] Univ Klin Giessen, Inst Biochem, Giessen, Germany

[3] Jomaa Pharmaka GmbH, D-35249 Giessen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(02)01003-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have developed the [5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for antimalarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The triauoromethyl substituted derivative displayed an IC50 of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：361 / 363

页数：3

共 11 条

[1] Antimalarial activity of 77 phospholipid polar head analogs:: Close correlation between inhibition of phospholipid metabolism and in vitro Plasmodium falciparum growth [J].