Bioisosteric replacement based on 1,2,4-oxadiazoles in the discovery of 1H-indazole-bearing neuroprotective MAO B inhibitors.
1,2,4-Oxadiazole
1H-indazole
Bioisostere
Monoamine oxidases
Neuroprotection
Tight-binder
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:
05 Jul 2023
05 Jul 2023
Historique:
received:
14
02
2023
revised:
03
04
2023
accepted:
04
04
2023
medline:
22
5
2023
pubmed:
14
5
2023
entrez:
13
5
2023
Statut:
ppublish
Résumé
Following a hybridization strategy, a series of 5-substituted-1H-indazoles were designed and evaluated in vitro as inhibitors of human monoamine oxidase (hMAO) A and B. Among structural modifications, the bioisostere-based introduction of 1,2,4-oxadiazole ring returned the most potent and selective human MAO B inhibitor (compound 20, IC
Identifiants
pubmed: 37178666
pii: S0223-5234(23)00318-5
doi: 10.1016/j.ejmech.2023.115352
pii:
doi:
Substances chimiques
Indazoles
0
Oxadiazoles
0
Hydrogen Peroxide
BBX060AN9V
Monoamine Oxidase
EC 1.4.3.4
Monoamine Oxidase Inhibitors
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115352Informations de copyright
Copyright © 2023 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.