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A New Series of M3 Muscarinic Antagonists Based on the 4-Amino-piperidine Scaffold.

✍ Scribed by O. Diouf; S. Gadeau; F. Chelle; M. Gelbcke; P. Talaga; B. Christophe; M. Gillard; R. Massingham; M. Guyaux

Publisher
John Wiley and Sons
Year
2003
Weight
113 KB
Volume
34
Category
Article
ISSN
0931-7597

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✦ Synopsis

A New Series of M3 Muscarinic Antagonists Based on the 4-Amino-piperidine Scaffold. -Twenty-five new N,N-disubstituted 4-aminopiperidines are synthesized by chemical modulation of aminopiperidine bearing a phenyl and a benzoyl group at the amino group. The main pharmacophoric pattern which allows a good affinity for the M3 muscarinic receptor consists of two aromatic groups linked to a basic nitrogen via a piperidine containing spacer. The basic nitrogen is necessarily linked to a lipophilic group such as benzyl or isoprenyl. The new family exhibits a binding selectivity for human M3 over M2 muscarinic receptors. Compound (Vc) shows potent anticholinergic properties and tissue selectivity. -(

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