4.5 Article

Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 5, Pages 1307-1311

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.033

Keywords

mGluR5; fenobam; anxiety; MPEP; pharmacophore

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Optimization of affinity and microsomal stability led to identification of the potent, metabolically stable fenobam analog 41. Robust in vivo efficacy of 41 was demonstrated in four different models of anxiety. Additionally, a ligand based pharmacophore alignment of fenobant and MPEP is proposed. (c) 2007 Elsevier Ltd. All rights reserved.

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