1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists

The structure–activity relationships of novel 1,5-benzodioxepin derivatives as muscarinic M1–M3 receptor antagonists are reported. Some of these compounds were found to possess high binding affinity for the muscarinic M3 receptor and potent effect on rhythmic increase in bladder pressure in unanesthetized rats following oral administration. These compounds displayed selectivity for the bladder over the salivary gland.

Graphical abstractThe structure–activity relationships of novel 1,5-benzodioxepin derivatives as muscarinic M1–M3 receptor antagonists are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide