Anti-malarial activity of N6-substituted adenosine derivatives.: Part I

被引：31
|
作者：
Golisade, A
Wiesner, J
Herforth, C
Jomaa, H
Link, A
机构：
[1] Univ Hamburg, Inst Pharm, D-20146 Hamburg, Germany
[2] Jomaa Pharmaka GmbH, D-35392 Giessen, Germany
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 03期
关键词：
D O I：
10.1016/S0968-0896(01)00331-5
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：
The synthesis and biological evaluation of novel N-6-substituted adenosine derivatives is reported. The first series of compounds was obtained using an established procedure for the nucleophilic substitution of a 1-(6-chloro-purin-9-yl)-beta-D-1-deoxyribofuranose with various amines. In addition, attachment of two different amino-functionalised spacer arms at the N-6-position of adenosine enabled derivatisation by an innovative polymer-assisted protocol. Thus, we were able to prepare three series of substituted derivatives that displayed activity versus the multiresistant Plasmodium falciparum strain Dd2 in cell culture experiments. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：769 / 777
页数：9
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