Himbacine analogs as muscarinic receptor antagonists-effects of tether and heterocyclic variations
Himbacine analogs as muscarinic receptor antagonists-effects of tether and heterocyclic variations
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DOI：
10.1016/j.bmcl.2004.05.047
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发表时间：
2004-08-02
影响因子：
2.7
通讯作者：
Ruperto, V
中科院分区：
文献类型：
--
作者：
Chackalamannil, S;Doller, D;Ruperto, V
采用杂环单元和将杂环单元连接到三环基序的系链的变化来合成天然产物喜巴辛的许多类似物。这些类似物中的几种具有与himbacine相当的M-2亲和力和M-1/M-2选择性。根据这些数据的结构和立体化学的要求，毒蕈碱结合的杂环单元进行了讨论。(C)2004 Elsevier Ltd.保留所有权利。
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.