Discovery of new chemical leads for selective EP1 receptor antagonists

A series of 4-({2-[alkyl(phenylsulfonyl)amino]phenoxy}methyl)benzoic acids were identified as functional PGE2 antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21–23 is presented here and structure–activity relationships (SAR) are also discussed.

Discovery process of new selective EP1 receptor antagonists 21–23 starting from 1.Figure optionsDownload as PowerPoint slide