Design, synthesis and evaluation of 2-(indolylmethylidene)-2,3-dihydro-1-benzofuran-3-one and 2-(indolyl)-4H-chromen-4-one derivatives as novel monoamine oxidases inhibitors.
Benzofurans
/ chemical synthesis
Benzopyrans
/ chemical synthesis
Dose-Response Relationship, Drug
Drug Design
Humans
Molecular Docking Simulation
Molecular Structure
Monoamine Oxidase
/ metabolism
Monoamine Oxidase Inhibitors
/ chemical synthesis
Recombinant Proteins
/ metabolism
Structure-Activity Relationship
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
06 2019
06 2019
Historique:
received:
07
01
2019
revised:
09
03
2019
accepted:
15
03
2019
pubmed:
2
4
2019
medline:
23
9
2020
entrez:
2
4
2019
Statut:
ppublish
Résumé
A series of 2-(indolylmethylidene)-2,3-dihydro-1-benzofuran-3-ones (aurone-indole hybrids) and 2-(indolyl)-4H-chromen-4-ones (flavone-indole hybrids) were designed, synthesized, and their monoamine oxidase (MAO) A and B inhibitory activities were evaluated. Compounds 5b and 11b showed potent inhibitory activities against MAO-A, comparable to that of pargyline used as a positive control, and most of the compounds, except for 2a and 10b, showed potent inhibitory activities against MAO-B. Compound 9a was the most potent and highly selective inhibitor of MAO-B (IC
Identifiants
pubmed: 30933784
pii: S0045-2068(19)30022-7
doi: 10.1016/j.bioorg.2019.03.042
pii:
doi:
Substances chimiques
Benzofurans
0
Benzopyrans
0
Monoamine Oxidase Inhibitors
0
Recombinant Proteins
0
Monoamine Oxidase
EC 1.4.3.4
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
594-600Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.