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Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6. Epub 2006 Dec 15.

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

Author information

1
Pharmaceutical Division, Discovery Research, F. Hoffmann-La Roche Ltd,CH-4070 Basel, Switzerland. Simona_m.ceccarelli@roche.com

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.

PMID:
17189691
DOI:
10.1016/j.bmcl.2006.12.006
[Indexed for MEDLINE]

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