作为选择性非竞争性代谢型谷氨酸受体1拮抗剂的2,4-二羧基吡咯：3,5-二甲基吡咯-2,4-二羧酸2-丙酯4-(1,2,2-三甲基丙基)酯的进一步表征及构效关系
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.
作者信息
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
机构信息
GlaxoSmithKline Medicine Research Centre, Via Fleming 4, 37135, Verona, Italy.
出版信息
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2113-8. doi: 10.1016/s0960-894x(03)00396-2.
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.
在3,5-二甲基吡咯-2,4-二羧酸2-丙酯4-(1,2,2-三甲基丙基)酯[3,5-二甲基PPP]作为一种强效且选择性的mGluR1非竞争性拮抗剂被披露之后，我们在此报告该重要工具的进一步体内特性，并揭示对C-5位的研究，这产生了非常强效的化合物。
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