Title of article :
A novel class of positive allosteric modulators of AMPA receptors: Design, synthesis, and structure–activity relationships of 3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrole-2-carboxylic acid, LY2059346
Author/Authors :
Hamideh Zarrinmayeh، نويسنده , , Eric Tromiczak، نويسنده , , Dennis M. Zimmerman، نويسنده , , Nancy Rankl، نويسنده , , Ken H. Ho، نويسنده , , Esteban Dominguez، نويسنده , , Ana Casta?o، نويسنده , , Ana Escribano، نويسنده , , Carmen Fernandez، نويسنده , , Alma Jimenez، نويسنده , , William J. Hornback، نويسنده , , Eric S. Nisenbaum، نويسنده ,
Abstract :
The synthesis and structure–activity relationship (SAR) of novel and highly potent positive allosteric modulators of AMPA receptors, 3-biphenyl-4-yl-4-cyano-5-ethyl-1-methyl-1H-pyrrole-2-carboxylic acid, are described. These studies indicated that higher potency was achieved with ortho substitution of the distal (D) phenyl of the 3-biphenyl ring and resulted in the discovery of a potent pyrrole LY2059346 (23q), that was selected for further evaluation in in vitro native tissue assays and in vivo experiments.
