Substituted 2-Aminothiopen-derivatives: A potential new class of GluR6-Antagonists

被引：45

作者：

Briel, D. ^{[1
]}

Rybak, A. ^{[1
]}

Kronbach, C. ^{[2
]}

Unverferth, K. ^{[2
]}

机构：

[1] Univ Leipzig, Fak Biowissensch Pharm & Psychol, Inst Pharm, D-04103 Leipzig, Germany

[2] Biotie Therapies GmbH, Radebeul, Germany

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 01期

关键词：

2-Aminothiophenes; Thieno[2,3-d]pyrimidines; Kainate receptor; Antiepileptics; Glutamate; HETEROCYCLIC SYNTHESIS; KAINATE RECEPTORS; NITRILES;

D O I：

10.1016/j.ejmech.2009.09.025

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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, Sa,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 mu M at the GluR6 receptor. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：69 / 77

页数：9

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