Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists

被引：54
|
作者：
Doller, D [1 ]
Chackalamannil, S [1 ]
Czarniecki, M [1 ]
McQuade, R [1 ]
Ruperto, V [1 ]
机构：
[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 06期
关键词：
D O I：
10.1016/S0960-894X(99)00101-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A parallel synthesis of racemic himbacine analogs was carried out by N-alkylation of various commercially available cyclic amine derivatives with the alkylating agent 4 which bears the tricyclic unit of himbacine. Several of these analogs have potency comparable to that of himbacine, albeit lacking the desired selectivity. Structure-activity relationship studies support the existence of a hydrophobic pocket in the receptor where the piperidine ring of dihydrohimbacine binds. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：901 / 906
页数：6
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