Discovery of novel 1-azoniabicyclo [2.2. 2] octane muscarinic acetylcholine receptor antagonists

…, B Underwood, J Dufour, KL Widdowson…

文献索引：Laine, Dramane I.; McCleland, Brent; Thomas, Sonia; Neipp, Christopher; Underwood, Brian; Dufour, Jeremy; Widdowson, Katherine L.; Palovich, Michael R.; Blaney, Frank E.; Foley, James J.; Webb, Edward F.; Luttmann, Mark A.; Burman, Miriam; Belmonte, Kristen; Salmon, Michael Journal of Medicinal Chemistry, 2009 , vol. 52, # 8 p. 2493 - 2505

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被引用次数: 15

摘要

A novel 4-hydroxyl (diphenyl) methyl substituted quinuclidine series was discovered as a very promising class of muscarinic antagonists. The structure− activity relationships of the connectivity of the diphenyl moiety to the quinuclidine core and around the ring nitrogen side chain are described. Computational docking studies using an homology model of the M3 receptor readily explained the observed structure− activity relationship of the various ...