Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.

Jean-Philippe Starck,Patrice Talaga,Luc Quéré,Philippe Collart,Bernard Christophe,Patrick Lo Brutto,Sophie Jadot,Dinesh Chimmanamada,Matteo Zanda,Alain Wagner, Charles Mioskowski,Roy Massingham,Michel Guyaux

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

The synthesis and biological evaluation of a novel family of M3 muscarinic antagonists are described. A systematic modification of the substituents to a novel alkyne-quinuclidine scaffold yielded original compounds displaying potent in vitro anticholinergic properties.

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关键词

Muscarinic receptor(s),Bladder,Urinary incontinence,Quinuclidine,Muscarinic antagonist(s),Overactive bladder

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