- 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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- Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: Identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase
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The four isomers of 4-aminopyrrolidine-2,4-dicarboxylate (APDC) were prepared and evaluated for their effects at glutamate receptors in vitro. (2R,4R)-APDC (2a), an aza analog of the nonselective mGluR agonist (1S,3R)- 1-aminocyclopentane-1,3-dicarboxylat
- Monn, James A.,Valli, Matthew J.,Johnson, Bryan G.,Salhoff, Craig R.,Wright, Rebecca A.,Howe, Trevor,Bond, Ann,Lodge, David,Spangle, Larry A.,Paschal, Jonathan W.,Campbell, Jack B.,Griffey, Kelly,Tizzano, Joseph P.,Schoepp, Darryle D.
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p. 2990 - 3000
(2007/10/03)
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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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- PYRROLIDINYL DI-CARBOXYLIC ACID DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS
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The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
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