Title of article :
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
Author/Authors :
Maria-Carmen Fernandez، نويسنده , , Ana Casta?o، نويسنده , , Esteban Dominguez، نويسنده , , Ana Escribano، نويسنده , , Delu Jiang، نويسنده , , Alma Jimenez، نويسنده , , Eric Hong، نويسنده , , William J. Hornback، نويسنده , , Eric S. Nisenbaum، نويسنده , , Nancy Rankl، نويسنده , , Eric Tromiczak، نويسنده , , Grant Vaught، نويسنده , , Hamideh Zarrinmayeh، نويسنده , , Dennis M. Zimmerman، نويسنده ,
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.
