Synthesis and metabotropic glutamate receptor antagonist activity of N 1-substituted analogs of 2R, 4R-4-aminopyrrolidine-2, 4-dicarboxylic acid

MJ Valli, DD Schoepp, RA Wright, BG Johnson…

文献索引：Valli, Matthew J.; Schoepp, Darryle D.; Wright, Rebecca A.; Johnson, Bryan G.; Kingston, Ann E.; Tomlinson, Rosemarie; Monn, James A. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1985 - 1990

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被引用次数: 15

摘要

A series of 1N-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 1N position of 2R, 4R-APDC resulted in the identification of a number of selective group II mGluR antagonists.