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.

An extensive SAR study of a series of aspartic and 2,3-diaminopropionic acid amides led to the discovery of 2-bromo-4,5-difluorophenoxy)phenyl]-l-asparagine—one of the most potent, selective, competitive non-substrate inhibitors of EAAT-2 identified to date.