Chackalamannil Samuel, Doller Darío, McQuade Robert, Ruperto Vilma
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70. doi: 10.1016/j.bmcl.2004.05.047.
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.
利用杂环单元以及连接杂环单元与三环基序的连接链上的变化，合成了多种天然产物海巴辛的类似物。其中一些类似物具有与海巴辛相当的M(2)亲和力和M(1)/M(2)选择性。根据这些数据讨论了毒蕈碱结合的杂环单元的结构和立体化学要求。
