β-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs).


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
12 Nov 2020
Historique:
received: 22 06 2020
accepted: 26 08 2020
entrez: 20 11 2020
pubmed: 21 11 2020
medline: 21 11 2020
Statut: epublish

Résumé

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

Identifiants

pubmed: 33214831
doi: 10.1021/acsmedchemlett.0c00342
pmc: PMC7667874
doi:

Types de publication

Journal Article

Langues

eng

Pagination

2212-2220

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Na Liu (N)

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark.

Anders A Jensen (AA)

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark.

Lennart Bunch (L)

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen, Denmark.

Classifications MeSH