Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid

Article abstract of DOI:10.1016/S0960-894X(98)00352-7

A series of N¹-substituted derivatives of (2R,4R)-4-aminopyrrolidine- 2,4-dicarboxylate (2R,4R-APDC) has been prepared as constrained analogs of γ-substituted glutamic acids and examined for their effects at recombinant metabotropic glutamate receptor (mGluR) subtypes in vitro. Appropriate substitution of the N¹ position of 2R,4R-APDC resulted in the identification of a number of selective group II mGluR antagonists.