Details

Autor(en) / Beteiligte

• Curtis, Neil R.
• Kulagowski, Janusz J.
• Leeson, Paul D.
• Mawer, Ian M.
• Ridgill, Mark P.
• Rowley, Michael
• Grimwood, Sarah
• Marshall, George R.

Titel

Synthesis and SAR of diiodotyrosine-derived glycine-site N-methyl- D-aspartate receptor ligands

Ist Teil von

• Bioorganic & medicinal chemistry letters, 1996-05, Vol.6 (10), p.1145-1150

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

1996

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• A series of analogues of the novel diiodotyrosine derived NMDA glycine-site ligand (R)-4 was prepared in which the aryl substitution, chain length and amino acid groups were varied. The key structural features for binding are the α-amino acid function, having the ( R) absolute stereochemistry, the 3,5-diiodo substituted aromatic ring and a lipophilic group attached at the phenolic oxygen of the tyrosine moiety. Analogues of the novel diiodotyrosine derived NMDA glycine-site ligand (R)-4 (IC 50 0.43μM vs [ 3H]L-689,560) were prepared in which the aryl substitution, chain length and amino acid groups were varied. The key structural features for binding are the α-amino acid function, having the ( R) absolute stereochemistry, the 3,5-diiodo substituted aromatic ring and a lipophilic group attached at the phenolic oxygen of the tyrosine moiety.