Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists

被引：5
|
作者：
Stark, H
Ligneau, X
Sadek, B
Ganellin, CR
Arrang, JM
Schwartz, JC
Schunack, W
机构：
[1] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany
[2] Lab Bioprojet, F-75003 Paris, France
[3] UCL, Christopher Ingold Labs, London WC1H 0AJ, England
[4] INSERM, Unite Neurobiol & Pharmacol Mol, U109, F-75014 Paris, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(00)00473-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel derivatives of the highly potent and selective histamine H-3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2379 / 2382
页数：4
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