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Bioorg Med Chem Lett. 2001 Apr 9;11(7):891-4.

Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.

Author information

1
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. yuguang.wang@spcorp.com

Abstract

Novel, selective M2 muscarinic antagonists, which replace the metabolically labile styrenyl moiety of the prototypical M2 antagonist 1 with an ether linkage, were synthesized. A detailed SAR study in this class of compounds has yielded highly active compounds that showed M2 Ki values of < 1.0 nM and >100-fold selectivity against M1, M3, and M5 receptors.

PMID:
11294385
DOI:
10.1016/s0960-894x(01)00100-7
[Indexed for MEDLINE]

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