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

…, J Huwyler, S Kolczewski, JU Peters, E Prinssen…

Index: Ceccarelli, Simona M.; Jaeschke, Georg; Buettelmann, Bernd; Huwyler, Joerg; Kolczewski, Sabine; Peters, Jens-Uwe; Prinssen, Eric; Porter, Richard; Spooren, Will; Vieira, Eric Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1302 - 1306

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Citation Number: 19

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.