91391-97-8Relevant academic research and scientific papers
Substituted 2-Aminothiopen-derivatives: A potential new class of GluR6-Antagonists
Briel,Rybak,Kronbach,Unverferth
scheme or table, p. 69 - 77 (2010/03/24)
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 μM at the GluR6 receptor.
