Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists

Jaeschke, Georg and Porter, Richard and Büttelmann, Bernd and Ceccarelli, Simona M. and Guba, Wolfgang and Kuhn, Bernd and Kolczewski, Sabine and Huwyler, Jörg and Mutel, Vincent and Peters, Jens-Uwe and Ballard, Theresa and Prinssen, Eric and Vieira, Eric and Wichmann, Jürgen and Spooren, Will. (2007) Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 17 (5). pp. 1307-1311.

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Official URL: http://edoc.unibas.ch/54625/

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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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Technologie (Huwyler)
UniBasel Contributors:Huwyler, Jörg
Item Type:Article, refereed
Article Subtype:Research Article
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:28 Nov 2017 07:38
Deposited On:28 Nov 2017 07:38

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