A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). New glutamate and aspartate analogues as potential neuroprotective agents

G. Campiani, M. De Angelis, S. Armaroli, C. Fattorusso, B. Catalanotti, A. Ramunno, V. Nacci, E. Novellino, C. Grewer, D. Ionescu, T. Rauen, R. Griffiths, C. Sinclair, E. Fumagalli, T. Mennini

Research output: Contribution to journalArticle

Abstract

Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, and new glutamate (Glu) and aspartate (Asp) analogues have been synthesized. The analogues 1a and 3 represent novel lead compounds for the development of EAAT substrates and nontransportable inhibitors, selective for EAATs over iGluRs, as possible neuroprotective agents useful to minimize the progression of chronic or acute neurodegenerative diseases. The role played by the protonatable amine function in the interaction with EAATs has been discussed.

Original languageEnglish
Pages (from-to)2507-2510
Number of pages4
JournalJournal of Medicinal Chemistry
Volume44
Issue number16
DOIs
Publication statusPublished - Aug 2 2001

ASJC Scopus subject areas

  • Organic Chemistry

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    Campiani, G., De Angelis, M., Armaroli, S., Fattorusso, C., Catalanotti, B., Ramunno, A., Nacci, V., Novellino, E., Grewer, C., Ionescu, D., Rauen, T., Griffiths, R., Sinclair, C., Fumagalli, E., & Mennini, T. (2001). A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). New glutamate and aspartate analogues as potential neuroprotective agents. Journal of Medicinal Chemistry, 44(16), 2507-2510. https://doi.org/10.1021/jm015509z