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

Vieira, Eric

doi:10.1016/j.bmcl.2006.12.006

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

Date Issued

2007-01-01

Author(s)

Ceccarelli, Simona M.

Jaeschke, Georg

Buettelmann, Bernd

Huwyler, Jörg

Kolczewski, Sabine

Peters, Jens-Uwe

Prinssen, Eric

Porter, Richard

Spooren, Will

Vieira, Eric

DOI

10.1016/j.bmcl.2006.12.006

Abstract

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.