Design, Synthesis, and Structure−Activity Relationship of Tropane Muscarinic Acetylcholine Receptor Antagonists
Journal of Medicinal Chemistry2009Vol. 52(16), pp. 5241–5252
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Dramane I. Lainé, Zehong Wan, Hongxing Yan, Chongjie Zhu, Haibo Xie, Wei Fu, Jakob Busch‐Petersen, Christopher E. Neipp, Roderick Davis, Katherine L. Widdowson, Frank E. Blaney, James J. Foley, Alicia M. Bacon, Edward F. Webb, Mark A. Luttmann, Miriam Burman, Henry M. Sarau, M Salmon, Michael R. Palovich, Kristen E. Belmonte
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 M(3) 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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