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2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: an exploration of the role of the pyrrolic scaffold.

作者信息

Micheli Fabrizio, Di Fabio Romano, Cavanni Paolo, Donati Daniele, Faedo Stefania, Gehanne Sylvie, Maffeis Micaela, Marchioro Carla, Sabbatini Fabio Maria, Tarzia Giorgio, Tranquillini Maria Elvira, Viziano Monica

机构信息

GlaxoSmithkline Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy.

出版信息

Farmaco. 2003 Oct;58(10):1005-9. doi: 10.1016/S0014-827X(03)00112-5.

Abstract

Following the disclosure of 3-(1,2,2-trimethylpropyl) 4-[3,5-dimethyl-2-propyloxycarbonyl]pyrrolecarboxylate as a potent and selective mGluR1 non-competitive antagonist, the role and the importance of the pyrrole template were investigated. Different aromatic moieties were investigated as possible bio-isosteric replacement of the original scaffold and some of them were shown to be partially able to mimic the properties of the original pyrrole ring.

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