Identification of novel glycine sulfonamide antagonists for the EP1 receptor

A high-throughput screen targeting the EP1 receptor identified non-acidic glycine sulfonamide derivative 2a with a pKi of 6.2. Analogue synthesis allowed a thorough investigation of the structure–activity relationship (SAR) and led to a 100-fold increase in recombinant potency.

The discovery, synthesis, pharmacokinetic profile and structure–activity relationships of a novel series of non-acidic EP1 receptor antagonists are described.Figure optionsDownload as PowerPoint slide