2. Academic Validation
  3. 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

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

Affiliation

  • 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.

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