Synthesis and preliminary evaluation of trans-3,4-conformationally-restricted glutamate and pyroglutamate analogues as novel EAAT2 inhibitors

被引：9

作者：

Denton, TT

Seib, T

Bridges, RJ

Thompson, CM ^{[1
]}

机构：

[1] Univ Montana, Dept Chem, Missoula, MT 59812 USA

[2] Univ Montana, COBRE Ctr Struct & Funct Neurosci, Dept Pharmaceut Sci, Missoula, MT 59812 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(02)00520-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Select trans-4,5-[bi]cyclohexenylglutamic and pyroglutamic acids (3,4-substituted glutamates) were synthesized in three steps and were screened as potential inhibitors of the sodium dependent excitatory amino acid transporters 2 (EAAT2) and 3 (EAAT3), the chloride dependent glial cystine/glutamate exchanger system x(c)(-), and the glutamate vesicular transport system (VGLUT). Two glutamate analogues and one pyroglutamate analogue were found to inhibit EAAT2 with activity comparable to dihydrokainate. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3209 / 3213

页数：5

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