Development of novel pyrazole, imidazo[1,2-b]pyrazole, and pyrazolo[1,5-a]pyrimidine derivatives as a new class of COX-2 inhibitors with immunomodulatory potential.
Anti-inflammatory activity
DFT calculation
Molecular docking studies
Pro-inflammatory cytokine
Pyrazole and pyrazolo[1,5-a]pyrimidine
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 Mar 2023
05 Mar 2023
Historique:
received:
11
11
2022
revised:
15
01
2023
accepted:
17
01
2023
pubmed:
26
1
2023
medline:
25
2
2023
entrez:
25
1
2023
Statut:
ppublish
Résumé
Searching for new compounds with anti-inflammatory properties is a significant target since inflammation is a major cause of pain. A series of pyrazole, imidazopyrazolone, and pyrazolopyrimidine derivatives were designed and synthesized by reaction of 3,5-diamino-1H-pyrazole derivative with cyclic and acyclic carbonyl reagents. The structure of the newly synthesized derivatives were fully characterized using different spectroscopic data and elemental analysis, and therefore, evaluated as COX-2 inhibitors. The in vitro COX-2 activity of the tested derivatives 2-13 displayed moderate to good potency with two derivatives 8 and 13 that exhibiting high potency to COX-2 with IC
Identifiants
pubmed: 36696764
pii: S0223-5234(23)00053-3
doi: 10.1016/j.ejmech.2023.115138
pii:
doi:
Substances chimiques
Cyclooxygenase 2 Inhibitors
0
Celecoxib
JCX84Q7J1L
Cyclooxygenase 2
EC 1.14.99.1
Interleukin-6
0
Tumor Necrosis Factor-alpha
0
Pyrazoles
0
Pyrimidines
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115138Informations 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.