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Bioorg Med Chem Lett. 2007 Mar 1;17(5):1307-11. Epub 2006 Dec 15.

Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.

Author information

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

Abstract

Optimization of affinity and microsomal stability led to identification of the potent, metabolically stable fenobam analog 4l. Robust in vivo efficacy of 4l was demonstrated in four different models of anxiety. Additionally, a ligand based pharmacophore alignment of fenobam and MPEP is proposed.

PMID:
17196387
DOI:
10.1016/j.bmcl.2006.12.033
[Indexed for MEDLINE]

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