| 19616944 |
Wan Z, Laine DI, Yan H, Zhu C, Widdowson KL, Buckley PT, Burman M, Foley JJ, Sarau HM, Schmidt DB, Webb EF, Belmonte KE, Palovich M: Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo [3.2.1] octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2. Epub 2009 Jul 8.
Design and syntheses of a novel series of muscarinic antagonists are reported. These efforts have culminated in the discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo [3.2.1] octane bromide (4a) as a potent and pan-active muscarinic antagonist as well as a functionally active compound in a murine model of bronchoconstriction. The compound has also displayed pharmacokinetic characteristics suitable for inhaled delivery. |
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