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

被引：55

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

页码：901 / 906

页数：6

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