Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure |
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| Authors: | Ceccarelli Simona M Jaeschke Georg Buettelmann Bernd Huwyler Jörg Kolczewski Sabine Peters Jens-Uwe Prinssen Eric Porter Richard Spooren Will Vieira Eric |
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| Institution: | Pharmaceutical Division, Discovery Research, F. Hoffmann-La Roche Ltd,CH-4070 Basel, Switzerland. Simona_m.ceccarelli@roche.com |
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| Abstract: | A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam. Representative compounds from this class show favorable pharmacokinetic properties and are active in an in vivo model of anxiety. |
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