Thieno[2,3-d]pyrimidines as antagonists of the glutamate receptors

被引：4

作者：

Briel, D. ^{[1
]}

Rybak, A. ^{[1
]}

Kronbach, C. ^{[2
]}

Unverferth, K. ^{[2
]}

机构：

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

[2] Elb AG, Radebeul, Germany

来源：

PHARMAZIE | 2008年 / 63卷 / 11期

关键词：

D O I：

10.1691/ph.2008.8600

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Although the function of the kainate receptors in the brain is still not clear, they are increasingly defined as targets in the development of new classes of anti-epileptics. The thienopyrimidines described in this report were tested for their antagonistic effect at the kainate receptor subtypes GluR5 and GluR6. The highest effectiveness was obtained by a 4-ethoxy-thieno[2,3-d]pyrimidin with an IC(50) = 68 mu M at the GluR6 receptor.

引用

页码：823 / 826

页数：4

共 14 条

[1]

ALLGEIER H, 2006, Patent No. 2006010591

[2]

BOHLE M, 1998, METHODS ORGANIC CH B, V9

[3]

Recurrent mossy fibers establish aberrant kainate receptor-operated synapses on granule cells from epileptic rats [J].

Epsztein, J ;

Represa, A ;

Jorquera, I ;

Ben-Ari, Y ;

Crépel, V .

JOURNAL OF NEUROSCIENCE, 2005, 25 (36) :8229-8239

[4]

Design, synthesis and bioactivities of novel diarylthiophenes:: inhibitors of tumor necrosis factor-α (TNF-α) production [J].

Fujita, M ;

Hirayama, T ;

Ikeda, N .

BIOORGANIC & MEDICINAL CHEMISTRY, 2002, 10 (10) :3113-3122

[5]

Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists [J].

Galatsis, Paul ;

Yamagata, Koji ;

Wendt, John A. ;

Connolly, Cleo J. ;

Mickelson, John W. ;

Milbank, Jared B. J. ;

Bove, Susan E. ;

Knauer, Christopher S. ;

Brooker, Rachel M. ;

Augelli-Szafran, Corinne E. ;

Schwarz, Roy D. ;

Kinsora, Jack J. ;

Kilgore, Kenneth S. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (23) :6525-6528

[6]

KRONBACH C, 2002, THESIS U LEIPZIG

[7]

Thienopyrimidines: synthesis, properties, and biological activity [J].

Litvinov, VP .

RUSSIAN CHEMICAL BULLETIN, 2004, 53 (03) :487-516

[8]

Mkrtchyan A.P., 2002, CHEM HETEROCYCL COMP, V38, P238

[9]

THIENO[2,3-D]PYRIMIDINES AS POTENTIAL CHEMOTHERAPEUTIC-AGENTS [J].

RAM, VJ .

ARCHIV DER PHARMAZIE, 1979, 312 (01) :19-25

[10]

RAM VJ, 1981, J HETEROCYCLIC CHEM, V18, P1277

← 1 2 →