Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.


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:
14 May 2020
Historique:
received: 13 11 2019
accepted: 16 12 2019
entrez: 22 5 2020
pubmed: 22 5 2020
medline: 22 5 2020
Statut: epublish

Résumé

Among several potential applications, sigma receptor ligands can be used as antipsychotics, antiamnesics, and against other neurodegenerative disorders as well as neuroprotective agents. We present herein a new series of diazepane-containing derivatives as σR ligands obtained by a conformational expansion approach of our previously synthesized piperidine-based compounds. The best results were reached by benzofurane

Identifiants

pubmed: 32435366
doi: 10.1021/acsmedchemlett.9b00524
pmc: PMC7236030
doi:

Types de publication

Journal Article

Langues

eng

Pagination

651-656

Informations de copyright

Copyright © 2019 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Daniele Zampieri (D)

Department of Chemical and Pharmaceutical Sciences, P.le Europa 1-Via Giorgieri 1, University of Trieste, 34127 Trieste, Italy.

Sara Fortuna (S)

Department of Chemical and Pharmaceutical Sciences, P.le Europa 1-Via Giorgieri 1, University of Trieste, 34127 Trieste, Italy.

Antonella Calabretti (A)

Department of Chemical and Pharmaceutical Sciences, P.le Europa 1-Via Giorgieri 1, University of Trieste, 34127 Trieste, Italy.

Maurizio Romano (M)

Department of Life Sciences, Via Valerio 28/1, University of Trieste, 34127 Trieste, Italy.

Renzo Menegazzi (R)

Department of Life Sciences, Via Valerio 28/1, University of Trieste, 34127 Trieste, Italy.

Dirk Schepmann (D)

Institute of Pharmaceutical and Medicinal Chemistry, Corrensstraße 48, 48149 Münster, Germany.

Bernhard Wünsch (B)

Institute of Pharmaceutical and Medicinal Chemistry, Corrensstraße 48, 48149 Münster, Germany.

Maria Grazia Mamolo (MG)

Department of Chemical and Pharmaceutical Sciences, P.le Europa 1-Via Giorgieri 1, University of Trieste, 34127 Trieste, Italy.

Classifications MeSH