Synthesis, in vitro and in vivo characterization of new benzoxazole and benzothiazole-based sigma receptor ligands.

Analgesics / chemical synthesis Animals Apoptosis / drug effects Benzothiazoles / chemical synthesis Benzoxazoles / chemical synthesis Humans Ligands MCF-7 Cells Mice Molecular Structure Receptors, sigma / agonists
Apoptosis Benzothiazole Benzoxazole Cancer Pain Sigma-1 receptors Sigma-2 receptors

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
15 Jul 2019
Historique:
received: 13 03 2019
revised: 18 04 2019
accepted: 19 04 2019
pubmed: 3 5 2019
medline: 18 6 2019
entrez: 3 5 2019
Statut: ppublish

Résumé

A new set of 5-chlorobenzoxazole- and 5-chlorobenzothiazole-based derivatives containing the azepane ring as a basic moiety was designed, synthesized and evaluated through binding assays to measure their affinity and selectivity towards σ

Identifiants

DOI: 10.1016/j.ejmech.2019.04.056 PMID: 31042618
pubmed: 31042618
pii: S0223-5234(19)30374-5
doi: 10.1016/j.ejmech.2019.04.056
pii:
doi:

Substances chimiques

Analgesics 0
Benzothiazoles 0
Benzoxazoles 0
Ligands 0
Receptors, sigma 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

226-235

Informations de copyright

Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Auteurs

Giuseppe Romeo (G)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Orazio Prezzavento (O)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy. Electronic address: prezzave@unict.it.

Sebastiano Intagliata (S)

Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, 32610, USA; Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy. Electronic address: s.intagliata@cop.ufl.edu.

Valeria Pittalà (V)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Maria N Modica (MN)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Agostino Marrazzo (A)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Rita Turnaturi (R)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Carmela Parenti (C)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Santina Chiechio (S)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy; Oasi Research Institute-IRCCS, Troina, Italy.

Emanuela Arena (E)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Agata Campisi (A)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Giovanni Sposito (G)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

Loredana Salerno (L)

Department of Drug Sciences, University of Catania, Viale A. Doria 6, 95125, Catania, Italy.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Analgésiques › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Eucaryotes › Animaux › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Mort cellulaire › Mort cellulaire régulée › Apoptose › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Benzothiazoles › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Benzoxazoles › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Cellules › Cellules cultivées › Lignée cellulaire › Cellules MCF-7 › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Synthesis, in vitro and in vivo...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur aux neuropeptides › Récepteurs aux opioïdes › Récepteur sigma › Synthesis, in vitro and in vivo...