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

Basic Information

ID: ALA1134751

Journal: Bioorg Med Chem Lett

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

Authors: Wang Y, Chackalamannil S, Chang W, Greenlee W, Ruperto V, Duffy RA, McQuade R, Lachowicz JE.

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.

CiteXplore: 11294385

DOI: 10.1016/s0960-894x(01)00100-7

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