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新型异噁唑啉基酸性氨基酸的合成及其对离子型谷氨酸受体亲和力和选择性的研究。

Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors.

机构信息

Dipartimento di Scienze Farmaceutiche Pietro Pratesi, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.

出版信息

Eur J Med Chem. 2011 Feb;46(2):787-93. doi: 10.1016/j.ejmech.2010.12.020. Epub 2010 Dec 23.

Abstract

The synthesis of four new isoxazoline-based amino acids being analogues of previously described glutamate receptor ligands is reported and their affinity for ionotropic glutamate receptors is analyzed in comparison with that of selected model compounds. Molecular modelling investigations have been carried out to rationalize the interaction with the NMDA receptors.

摘要

报告了四种新型异恶唑啉基氨基酸的合成,这些氨基酸是先前描述的谷氨酸受体配体的类似物,并分析了它们与选定模型化合物相比对离子型谷氨酸受体的亲和力。进行了分子建模研究,以合理化与 NMDA 受体的相互作用。

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