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 …
…, C Zhu, KL Widdowson, PT Buckley, M Burman…
Index: Wan, Zehong; Laine, Dramane I.; Yan, Hongxing; Zhu, Chongjie; Widdowson, Katherine L.; Buckley, Peter T.; Burman, Miriam; Foley, James J.; Sarau, Henry M.; Schmidt, Dulcie B.; Webb, Edward F.; Belmonte, Kristen E.; Palovich, Michael Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4560 - 4562
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Citation Number: 7
Abstract
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 ...
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