4.5 Article

Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 5, 页码 1307-1311

出版社

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

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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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