Rational design, synthesis, and structure–activity relationship of benzoxazolones: New potent mglu5 receptor antagonists based on the fenobam structure

A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam. Representative compounds from this class show favorable pharmacokinetic properties and are active in an in vivo model of anxiety.

A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam.Figure optionsDownload as PowerPoint slide