Discovery and structure–activity relationships of a novel series of benzopyran-based KATP openers for urge urinary incontinence

A novel series of benzopyran derivatives were synthesized and evaluated as KATP channel openers. Structure–activity relationships were investigated around 4-position of the benzopyran nucleus. Optimization of 4-substituent with some heterocyclic rings led to compound 13b bearing a benzo[d]isoxazol-3-one moiety as a potent and selective KATP channel opener in vitro. In two anesthetized rat models of myogenic bladder overactivity, compound 13b was found to inhibit spontaneous bladder contractions.

A novel series of benzopyran derivatives were synthesized and evaluated as KATP channel openers. The lead compound is a potent and selective KATP channel opener in vitro. In two anesthetized rat models of myogenic bladder overactivity, it is found to inhibit spontaneous bladder contractions.Figure optionsDownload as PowerPoint slide