363-16-6Relevant academic research and scientific papers
NOVEL ASPARTYLAMIDE INHIBITORS OF EXCITATORY AMINO ACID TRANSPORTERS
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, (2013/09/26)
The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodr
Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2
Greenfield, Alexander,Grosanu, Cristina,Dunlop, John,McIlvain, Beal,Carrick, Tikva,Jow, Brian,Lu, Qiang,Kowal, Dianne,Williams, John,Butera, John
, p. 4985 - 4988 (2007/10/03)
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 activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 ± 5 nM) and selective inhibitors of EAAT-2 identified to date.
