9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers |
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Authors: | Vieira Eric Huwyler Jörg Jolidon Synèse Knoflach Frédéric Mutel Vincent Wichmann Jürgen |
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Institution: | Pharma Division, Discovery Research, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. eric.vieira@roche.com |
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Abstract: | Small molecule mGluR1 enhancers based on the lead compound (9H-xanthene-9-carbonyl)-carbamic acid butyl ester derived from random-screening hit diphenylacetyl-carbamic acid ethyl ester were designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure-activity relationship of this new class of positive allosteric modulators of mGlu1 receptors will be discussed in detail. |
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