EXCITATORY AMINO-ACID RECEPTOR ANTAGONISTS - SYNTHESIS AND PHARMACOLOGY OF 3-(CARBOXYMETHOXY)ISOXAZOLES DERIVED FROM AMPA

被引：5

作者：

MADSEN, U

ANDRESEN, L

POULSEN, GA

RASMUSSEN, TB

EBERT, B

KROGSGAARDLARSEN, P

BREHM, L

机构：

[1] PharmaBiotec Research Center, Department of Organic Chemistry, Royal Danish School of Pharmacy, DK-2100 Copenhagen

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80035-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three acidic amino acids were synthesized using the non-NMDA antagonist, (RS)-2-amino-3-[3-(carboxymethoxy)-5-methyl-4-isoxazolyl]propionic acid (AMOA), as a lead structure. (RS)-3-(carboxymethoxy)-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid (1) was found to be a selective NMDA antagonist, whereas (RS)-2-amino-3-[3-(carboxymethoxy)-5-trifluoromethyl-4-isoxazolyl]propionic acid (2) was shown to be a non-NMDA antagonist.

引用

页码：1649 / 1654

页数：6

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