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
GlaxoSmithkline Medicine Research Centre, Via Fleming 4, 37135 Verona, Italy.
Farmaco. 2003 Oct;58(10):1005-9. doi: 10.1016/S0014-827X(03)00112-5.
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.