Synthesis and optimization of novel and selective muscarinic M3 receptor antagonists

A series of constrained piperidine analogues were synthesized as novel muscarinic M3 receptor antagonists. Evaluation of these compounds in binding assays revealed that they not only have high affinity for the M3 receptor but also have high selectivity over the M2 receptor.

Graphical abstractA series of constrained piperidine derivatives were synthesized as muscarinic M3 receptor antagonists. In vitro evaluation of these compounds reveals high affinity for the M3 receptor and high selectivity over the M2 receptor.Figure optionsDownload full-size imageDownload as PowerPoint slide