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ID: ALA1146878
Journal: Bioorg Med Chem Lett
Title: A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.
Authors: Fernandez MC, Castaño A, Dominguez E, Escribano A, Jiang D, Jimenez A, Hong E, Hornback WJ, Nisenbaum ES, Rankl N, Tromiczak E, Vaught G, Zarrinmayeh H, Zimmerman DM.
Abstract: The synthesis and initial SAR studies of novel, highly potent positive allosteric modulators of AMPA receptors based on 3-(4-tert-butylphenyl)-4-cyano-5-methylsulfanyl-thiophene-2-carboxylic acid (6a) are described. SAR studies at the thioether moiety indicated that substitution at this position was mandatory and better potency was achieved with small groups.
CiteXplore: 16879964