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- W3082232241 abstract "The excitatory amino acid transporters (EAATs) mediate uptake of the major excitatory neurotransmitter l-glutamate (Glu). The essential functions governed by these transporters in regulating the central Glu level make them interesting therapeutic targets in a wide range of neurodegenerative and psychiatric disorders. l-Aspartate (Asp), another EAAT substrate, has served as a privileged scaffold for the development of EAAT inhibitors. In this study, we designed and synthesized the first β-indolyloxy Asp analogs 15a-d with the aim to probe a hitherto unexplored adjacent pocket to the substrate binding site. The pharmacological properties of 15a-d were characterized at hEAAT1-3 and rEAAT4 in a conventional [3H]-d-Asp uptake assay. Notably, thiophene analog 15b and the para-trifluoromethyl phenyl analog 15d were found to be hEAAT1,2-preferring inhibitors exhibiting IC50 values in the high nanomolar range (0.21-0.71 μM) at these two transporters versus IC50 values in the low micromolar range at EAAT3,4 (1.6-8.9 μM). In summary, the results presented herein open up for further structure-activity relationship studies of this new scaffold." @default.
- W3082232241 created "2020-09-08" @default.
- W3082232241 creator A5020642089 @default.
- W3082232241 creator A5053231387 @default.
- W3082232241 creator A5058963077 @default.
- W3082232241 date "2020-09-01" @default.
- W3082232241 modified "2023-10-02" @default.
- W3082232241 title "β-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs)" @default.
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- W3082232241 doi "https://doi.org/10.1021/acsmedchemlett.0c00342" @default.
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