Title of article :
Rational design, synthesis, and structure–activity relationship of benzoxazolones: New potent mglu5 receptor antagonists based on the fenobam structure
Author/Authors :
Simona M. Ceccarelli، نويسنده , , Georg Jaeschke، نويسنده , , Bernd Buettelmann، نويسنده , , J?rg Huwyler، نويسنده , , Sabine Kolczewski، نويسنده , , Jens-Uwe Peters، نويسنده , , Eric Prinssen، نويسنده , , Richard Porter، نويسنده , , Will Spooren، نويسنده , , Eric Vieira، نويسنده ,
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.
Keywords :
Fenobam , Anxiety , MPEP , Benzoxazolone , mGluR5
