Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.
Basic Information
ID: ALA1154608
Journal: Eur J Med Chem
Title: Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.
Authors: Briel D, Rybak A, Kronbach C, Unverferth K.
Abstract: In the course of search for new therapeutic agents against epilepsy new inhibitors for the kainate receptor subtypes GluR5 and GluR6 were synthesized. We were able to synthesize new substituted thieno[2,3-d]pyrimidines 3a,b, 4a,b, 5a,b as well as thiophene-3-carboxamides 2a-d and a multitude of substituted 4-methyl-5-phenylthiophene-3-carboxylic acids. All compounds described herein were tested for their antagonistic effect towards the kainate receptor subtypes GluR5 and GluR6. The highest activity was observed for ethyl 2-amino-4-methyl-5-phenylthiophene-3-carboxylate 1c with an IC50=0.75 microM at the GluR6 receptor.
CiteXplore: 19819046
DOI: 10.1016/j.ejmech.2009.09.025
Patent ID: ┄