Discovery of novel indole-based aroylhydrazones as anticonvulsants: Pharmacophore-based design.
Anticonvulsants
Hepatotoxicity
Melatonin derivatives
Neurotoxicity
Rodents
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
09 2019
09 2019
Historique:
received:
11
01
2019
revised:
29
05
2019
accepted:
31
05
2019
pubmed:
21
6
2019
medline:
21
10
2020
entrez:
21
6
2019
Statut:
ppublish
Résumé
A number of novel melatonin derivatives, containing aroylhydrazone moieties, were synthesized and explored in vivo for anticonvulsant activity, neurotoxicity in ICR mice as well as in-vitro for cytoxicity and oxidative stress in rats. The structures and configurations were confirmed by NMR, FTIR, HRMS and crystal X-ray diffraction method. For selection of potent structures for synthesis a pharmacophore model was used. Two compounds 3e, with a 2-furyl moiety fragment and 3f with 2-thienyl fragment, showed a potency in maximal electroshock (MES) test (ED
Identifiants
pubmed: 31220672
pii: S0045-2068(19)30055-0
doi: 10.1016/j.bioorg.2019.103028
pii:
doi:
Substances chimiques
Anticonvulsants
0
Hydrazones
0
Melatonin
JL5DK93RCL
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103028Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.