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Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70.

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

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  • 1Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.


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.

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