- Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid
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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.
- Valli, Matthew J.,Schoepp, Darryle D.,Wright, Rebecca A.,Johnson, Bryan G.,Kingston, Ann E.,Tomlinson, Rosemarie,Monn, James A.
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p. 1985 - 1990
(2007/10/03)
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- Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC - an apparent mGluR6 selective ligand
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The synthesis of the 1-benzyl derivative of (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid (1-benzyl-APDC) starting from cis-4-hydroxy-D-proline is disclosed together with a study of the activity of this compound at metabotropic glutamate receptors (mGl
- Tueckmantel, Werner,Kozikowski, Alan P.,Wang, Shaomeng,Pshenichkin, Sergey,Wroblewski, Jarda T.
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p. 601 - 606
(2007/10/03)
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- Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor antagonists
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The present invention provides pyrrolidinyl di-carboxylic acid derivatives that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders. This invention further provides novel pyrr
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- Asymmetric syntheses of all four isomers of 4-amino-4-carboxyproline: Novel conformationally restricted glutamic acid analogues
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Asymmetric syntheses of all four isomers of 4-amino-4-carboxyprolines, i.e. (2S,4S)-3, (2S,4R)-4, and their corresponding enantiomers, as novel conformationally restricted analogues of glutamic acid, were performed from trans-4-hydroxy-L-proline as a homochiral starting material. The key step was the spirohydantoin ring formation by employing the Bucherer-Bergs reaction of 4-oxoproline derivatives. These structures were determined by NMR studies.
- Tanaka,Sawanishi
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p. 1641 - 1656
(2007/10/02)
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