Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate …

A Greenfield, C Grosanu, J Dunlop, B McIlvain…

Index: Greenfield, Alexander; Grosanu, Cristina; Dunlop, John; McIlvain, Beal; Carrick, Tikva; Jow, Brian; Lu, Qiang; Kowal, Dianne; Williams, John; Butera, John Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4985 - 4988

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Citation Number: 18

Abstract

Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological ...