Design, synthesis and activity of novel derivatives of Oxybutynin and Tolterodine

Novel derivatives of Tolterodine (1) and Oxybutynin (2) have been designed using conformationally restricted azabicyclics as replacement for open-chain amines. The synthesis and structure–activity relationships are presented.

Graphical abstractNovel analogues of Tolterodine and Oxybutynin are reported using 3-azabicyclo[3.1.0]hexane. The synthesis and SAR highlights our efforts to synthesize a bladder selective muscarinic receptor antagonist.Figure optionsDownload full-size imageDownload as PowerPoint slide