Design, synthesis, and structure− activity relationship of tropane muscarinic acetylcholine receptor antagonists
…, H Xie, W Fu, J Busch-Petersen, C Neipp…
Index: Laine, Dramane I.; Wan, Zehong; Yan, Hongxing; Zhu, Chongjie; Xie, Haibo; Fu, Wei; Busch-Petersen, Jakob; Neipp, Christopher; Davis, Roderick; Widdowson, Katherine L.; Blaney, Frank E.; Foley, James; Bacon, Alicia M.; Webb, Edward F.; Luttmann, Mark A.; Burman, Miriam; Sarau, Henry M.; Salmon, Michael; Palovich, Michael R.; Belmonte, Kristen Journal of Medicinal Chemistry, 2009 , vol. 52, # 16 p. 5241 - 5252
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Citation Number: 10
Abstract
Novel tropane derivatives were characterized as muscarinic acetylcholine receptor antagonists (mAChRs). Through optimization of the structure− activity relationship around the tropane scaffold, the quaternary ammonium salt 34 was identified as a very potent M3 mAChR antagonist. The compound was functionally active and displayed greater than 24 h duration of action in a mouse model of bronchoconstriction.
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