Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists

  • Eur J Med Chem. 2010 Jan;45(1):69-77. doi: 10.1016/j.ejmech.2009.09.025.
D Briel  1 ,  A Rybak ,  C Kronbach ,  K Unverferth
Affiliations
  • 1. Pharmazeutische Chemie, Institut für Pharmazie, Fakultät für Biowissenschaften, Pharmazie und Psychologie, Universität Leipzig, Brüderstr. 34, 04103 Leipzig, Germany. [email protected]
PMID: 19819046 DOI: 10.1016/j.ejmech.2009.09.025
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.