Himbacine analogs as muscarinic receptor antagonists-effects of tether and heterocyclic variations

被引:11
作者
Chackalamannil, S [1 ]
Doller, D [1 ]
McQuade, R [1 ]
Ruperto, V [1 ]
机构
[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA
关键词
D O I
10.1016/j.bmcl.2004.05.047
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A number of analogs of the natural product himbacine were synthesized employing variations at the heterocyclic unit and the tether that links the heterocyclic unit to the tricyclic motif. Several of these analogs had M-2 affinity and M-1/M-2 selectivity comparable to those of himbacine. The structural and stereochemical requirements of the heterocyclic unit for muscarinic binding are discussed in the light of these data. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3967 / 3970
页数:4
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