Synthesis and Sar of Diiodotyrosine-Derived Glycine-Site N-Methyl-D-Aspartate Receptor Ligands

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.