3'-DISUBSTITUTED-2-(2'-CARBOXYCYCLOPROPYL)GLYCINES AS POTENT AND SELECTIVE ANTAGONISTS OF METABOTROPIC GLUTAMATE RECEPTORS

2-(9-Xanthylmethyl)-2-(2' -carboxycyclopropyl) glycine 6e is a novel m etabotropic glutamate receptor antagonist. A series of alpha, C-3' dis ubstituted (carboxycyclopropyl)glycines 6f-n were prepared. Antagonist activity was observed for all these compounds at group 2 and group 3 mGluRs. Although they were slightly less active on group 2 mGluRs than non C-3' substituted 6e, the compounds 6f-n were more selective with lesser or no activity on group I mGluR subtypes (IC50 values greater t han 100 mu m). (C) 1998 Elsevier Science Ltd. All rights reserved.