Anti-glycemic potential of benzophenone thio/semicarbazone derivatives: synthesis, enzyme inhibition and ligand docking studies.
Caco-2 cell line
Type 2 diabetes mellitus
benzophenone
dipeptidyl peptidase-IV (DPP-IV)
thiosemicarbazone
Journal
Journal of biomolecular structure & dynamics
ISSN: 1538-0254
Titre abrégé: J Biomol Struct Dyn
Pays: England
ID NLM: 8404176
Informations de publication
Date de publication:
10 2022
10 2022
Historique:
pubmed:
27
3
2021
medline:
14
9
2022
entrez:
26
3
2021
Statut:
ppublish
Résumé
Inhibition of dipeptidyl peptidase-IV (DPP-IV) has been identified as a promising approach for the treatment of type 2 diabetes mellitus (T2DM). Therefore, development of DPP-IV inhibitors with new chemical scaffold is of utmost importance to medicinal chemistry. In the present study, we identified benzophenone thio- and semicarbazone scaffolds as novel DPP-IV inhibitors. For that purpose, benzophenone thio- and semicarbazone were synthesized through a 2-step reaction. These newly synthetic derivatives were characterized by different spectroscopic techniques, including HREI-MS and NMR. whereas stereochemistry of the iminic bond was predicted by NOESY experiments. Thio- and semicarbazones derivatives were evaluated for their DPP-IV inhibitory potential and found to exhibit a good to moderate enzyme inhibitory activity. Most active and non-cytotoxic derivatives were further evaluated for their DPP-IV inhibitory potential in
Identifiants
pubmed: 33769204
doi: 10.1080/07391102.2021.1897045
doi:
Substances chimiques
Benzophenones
0
Blood Glucose
0
Dipeptidyl-Peptidase IV Inhibitors
0
Ligands
0
Semicarbazones
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM