2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships |
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| Authors: | Micheli Fabrizio Di Fabio Romano Bordi Fabio Cavallini Palmina Cavanni Paolo Donati Daniele Faedo Stefania Maffeis Micaela Sabbatini Fabio Maria Tarzia Giorgio Tranquillini Maria Elvira |
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| Institution: | GlaxoSmithKline Medicine Research Centre, Via Fleming 4, 37135, Verona, Italy. fabio@gsk.com |
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| Abstract: | Following the disclosure of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester 3,5-dimethyl PPP] as a potent and selective mGluR1 non-competitive antagonist, we report here further in vivo characterization of this important tool and disclose the investigation of the C-5 position, which led to very potent compounds. |
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