Synthesis, ADMT prediction, and
Journal
RSC advances
ISSN: 2046-2069
Titre abrégé: RSC Adv
Pays: England
ID NLM: 101581657
Informations de publication
Date de publication:
22 Jun 2023
22 Jun 2023
Historique:
received:
18
03
2023
accepted:
17
06
2023
medline:
28
6
2023
pubmed:
28
6
2023
entrez:
28
6
2023
Statut:
epublish
Résumé
In this work, a new series of quinoline-quinazolinone-thioacetamide derivatives 9a-p were designed using a combination of effective pharmacophores of the potent α-glucosidase inhibitors. These compounds were synthesized by simple chemical reactions and evaluated for their anti-α-glucosidase activity. Among the tested compounds, compounds 9a, 9f, 9g, 9j, 9k, and 9m demonstrated significant inhibition effects in comparison to the positive control acarbose. Particularly, compound 9g with inhibitory activity around 83-fold more than acarbose exhibited the best anti-α-glucosidase activity. Compound 9g showed a competitive type of inhibition in the kinetic study, and the molecular simulation studies demonstrated that this compound with a favorable binding energy occupied the active site of α-glucosidase. Furthermore,
Identifiants
pubmed: 37377867
doi: 10.1039/d3ra01790g
pii: d3ra01790g
pmc: PMC10291282
doi:
Types de publication
Journal Article
Langues
eng
Pagination
19243-19256Informations de copyright
This journal is © The Royal Society of Chemistry.
Déclaration de conflit d'intérêts
All the authors declare that they have no conflict of interest.
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