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Amidines Amidines Q 0500Novel N 1 -(Benzyl)cinnamamidine Derived NR2B Subtype-Selective NMDA Receptor Antagonists. -The synthesis of title compounds such as (V) and (X) by reaction of cinnamimidate (III) with the appropriate amine or via Horner-Wadsworth-Emmons reaction of an amidine phosphonate and their evaluation as NR2B subtype NMDA receptor ligands are described. Compound (Vb) showed excellent selectivity over NR2A (no yields given). -(CURTIS*, N. R.; DIGGLE, H. J.; KULAGOWSKI, J. J.; LONDON, C.; GRIMWOOD, S.; HUTSON, P. H.; MURRAY, F.; RICHARDS, P.; MACAULAY, A.; WAFFORD KEITH A.; Bioorg. Med. Chem. Lett. 13 (2003) 4, 693-696; Merck Sharp Dohme Res. Lab., Dep. Med. Chem., Neurosci. Res. Cent., Harlow, Essex CM20 2QR, UK; Eng.) -M. Schroeter 25-110

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7 Ligands. -On the basis of a hit from a screening program, a novel set of compounds such as (III), (VI), (IX) and (XI) is synthesized. The biological results are discussed in detail. The most interesting derivative is (VI) showing the desired biological profile. -(THOMSON*, C. G.; BEER, M. S.; CURTIS, N. R.; DIGGLE, H. J.; HANDFORD, E.; KULAGOWSKI, J.