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2004
Amino acids
U 0400
Stereoselective Synthesis and Preliminary Evaluation of New D-3-Heteroarylcaras Ligands of the NMDA Receptor. — The novel D-amino acids (X)
52- 169 bonylalanines
are designed as analogues of the antagonist MDL 100453 in which a methylenephosphonate moiety is substituted with a heteroaromatic group. Amino acids (X) are synthesized in enantiomerically pure form utilizing a syn-stereoselective conjugate addition of benzylamine (II) to enoate (I), prepared from D-mannitol, as a key step. Compounds (X) interact with NMDA receptors in distinct manners: (Xa) is a weak
non-competitive antagonist of NMDA receptors, it inhibits the binding of MK-801 in
an agonist-independent fashion, protects neurons from glutamate injury, and partially
blocks NMDA-evoked whole-cell currents while the main activity of (Xb) is a positive
modulation of the NMDA receptor, possibly through the allosteric glycine site. —
(LIMA, P. G.; CARUSO, R. R. B.; ALVES, S. O.; PESSOA, R. F.;
MENDONCA-SILVA, D. L.; NUNES, R. J.; NOEL, F.; CASTRO, N. G.; COSTA*, P.
R. R.; Bioorg. Med. Chem. Lett. 14 (2004) 17, 4399-4403; Lab. Quim. Bioorg., Nucl.
Pesqui. Prod. Nat., Univ. Fed. Rio de Janeiro, 21941 Rio de Janeiro, Brazil; Eng.) —
H. Hoennerscheid
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