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ID: ALA1130627

Journal: Bioorg Med Chem Lett

Title: 2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors.

Authors: Collado I, Ezquerra J, Mazón A, Pedregal C, Yruretagoyena B, Kingston AE, Tomlinson R, Wright RA, Johnson BG, Schoepp DD.

Abstract: 2-(9-Xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine 6e is a novel metabotropic glutamate receptor antagonist. A series of alpha, C-3' disubstituted (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 1 mGluR subtypes (IC50 values greater than 100 microns).

CiteXplore: 9873635

DOI: 10.1016/s0960-894x(98)00510-1