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Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists |
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| Authors: | Jaeschke Georg Porter Richard Büttelmann Bernd Ceccarelli Simona M Guba Wolfgang Kuhn Bernd Kolczewski Sabine Huwyler Jörg Mutel Vincent Peters Jens-Uwe Ballard Theresa Prinssen Eric Vieira Eric Wichmann Jürgen Spooren Will |
| Affiliation: | 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. |
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