A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold

…, F Chelle, M Gelbcke, P Talaga, B Christophe…

Index: Diouf; Gadeau; Chelle; Gelbcke; Talaga; Christophe; Gillard; Massingham; Guyaux Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 18 p. 2535 - 2539

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Citation Number: 11

Abstract

A series of 4-amino-piperidine containing molecules have been synthesized and structure– affinity relationship toward the M3-muscarinic receptor has been investigated. Chemical modulations provided molecules with Ki for the human M3-R up to 1 nM with variable selectivity (3-to 40-fold) over the human M2-R. Compounds 2 (pA2= 8.3, 8.6) demonstrates in vitro on guinea pig bladder and ileal strips potent anticholinergic properties and tissue ...