Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.
1,2,3-triazole analogues
Antidiabetic drugs
Computational simulations
DPP-4 inhibitors
Docking
MD simulations
Sitagliptin
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 01 2021
01 01 2021
Historique:
received:
17
04
2020
revised:
11
10
2020
accepted:
01
11
2020
pubmed:
21
11
2020
medline:
31
7
2021
entrez:
20
11
2020
Statut:
ppublish
Résumé
Novel 1,2,3-triazole analogues (S7 ~ S10) were synthesized and evaluated for their inhibitory activity against hDPP-4. All the 1,2,3-triazole analogues exhibited moderate in vitro hDPP-4 inhibitory activities (265 ~ 780 nM). These results are somewhat less potent compared to those of known 1,2,3-triazole analogues (S1 ~ S6, 14 ~ 254 nM). S2 and S3 manifested excellent potency against hDPP-4 with IC
Identifiants
pubmed: 33214038
pii: S0968-0896(20)30691-X
doi: 10.1016/j.bmc.2020.115861
pii:
doi:
Substances chimiques
Dipeptidyl-Peptidase IV Inhibitors
0
Triazoles
0
DPP4 protein, human
EC 3.4.14.5
Dipeptidyl Peptidase 4
EC 3.4.14.5
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
115861Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.