Synthesis of N(1)-substituted analogues of (2R,4R)-4-amino-pyrrolidine-2,4-dicarboxylic acid as agonists, partial agonists, and antagonists of group II metabotropic glutamate receptors

  • Bioorg Med Chem Lett. 2001 Jul 23;11(14):1919-24. doi: 10.1016/s0960-894x(01)00329-8.
J K Mukhopadhyaya  1 ,  A P Kozikowski ,  E Grajkowska ,  S Pshenichkin ,  J T Wroblewski
Affiliations
  • 1. Department of Neurology, Drug Discovery Program, Georgetown University Medical Center, 3900 Reservoir Road, N.W., 20007, Washington, DC, USA.
PMID: 11459661 DOI: 10.1016/s0960-894x(01)00329-8
Abstract

The chemical synthesis of a series of N(1)-substituted derivatives of (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid [(2R,4R)-APDC] as constrained analogues of gamma-substituted glutamic acids is described. Appropriate substitution of the N(1)-position results in agonist, partial agonist, or antagonist activity at mGluR2, mGluR3, and/or mGluR6.

Products