恶二唑烷二酮衍生物作为喹啉酸类似物的合成及其在大鼠海马体中喹啉酸敏感位点的评估。

Synthesis of oxadiazolidinedione derivatives as quisqualic acid analogues and their evaluation at a quisqualate-sensitized site in the rat hippocampus.

作者信息

Venkatraman S, Roon R J, Schulte M K, Koerner J F, Johnson R L

机构信息

Department of Medicinal Chemistry, College of Pharmacy, Medical School, University of Minnesota, Minneapolis 55455.

出版信息

J Med Chem. 1994 Nov 11;37(23):3939-46. doi: 10.1021/jm00049a013.

DOI:10.1021/jm00049a013

Abstract

The ability of quisqualic acid (1) to sensitize neurons to depolarization by omega-phosphono alpha-amino acid analogues of excitatory amino acids is a highly specific phenomenon and is termed the QUIS effect. In an attempt to elucidate the structure-activity relationships for this sensitization, analogues 2-6 of quisqualic acid have been synthesized. Compounds 4, 5, and 6 showed no quisqualate sensitization with respect to L-2-amino-6-phosphonohexanoic acid (L-AP6), while compounds 2 and 3 were 1/10 and 1/1000, respectively, as active as quisqualic acid in sensitizing neurons toward L-AP6.

摘要

使君子氨酸（1）对兴奋性氨基酸的ω-膦酰基α-氨基酸类似物引起的神经元去极化敏感的能力是一种高度特异性的现象，被称为QUIS效应。为了阐明这种敏感性的构效关系，已经合成了君子氨酸的类似物2-6。化合物4、5和6对L-2-氨基-6-膦酰基己酸（L-AP6）没有表现出对喹啉酸的敏感性，而化合物2和3在使神经元对L-AP6敏感方面的活性分别是君子氨酸的1/10和1/1000。

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Synthesis of oxadiazolidinedione derivatives as quisqualic acid analogues and their evaluation at a quisqualate-sensitized site in the rat hippocampus.恶二唑烷二酮衍生物作为喹啉酸类似物的合成及其在大鼠海马体中喹啉酸敏感位点的评估。

J Med Chem. 1994 Nov 11;37(23):3939-46. doi: 10.1021/jm00049a013.

2

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