Exploring of novel oxazolones and imidazolones as anti-inflammatory and analgesic candidates with cyclooxygenase inhibitory action.
Future Med Chem
; 16(10): 963-981, 2024.
Article
in En
| MEDLINE
| ID: mdl-38639393
ABSTRACT
Aim:
Over the last few decades, therapeutic needs have led to a search for safer COX-2 inhibitors with potential anti-inflammatory and analgesic activity. Materials &methods:
A new series of oxazolone and imidazolone derivatives 3a-c and 4a-r were synthesized and evaluated as anti-inflammatory and analgesic agents. COX-1/COX-2 isozyme selectivity testing and molecular docking were performed.Results:
All compounds showed good activities comparable to those of the reference, celecoxib. The most active compounds 3a, 4a, 4c, 4e and 4f showed promising gastric tolerability with an ulcer index lower than that of celecoxib. The molecular docking of p-methoxyphenyl derivative 4c showed alkyl interaction with the side pocket His75 of COX-2 and achieved the best anti-inflammatory activity, with a COX-2 selectivity index better than that of celecoxib.
[Box see text].
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oxazolone
/
Cyclooxygenase 1
/
Cyclooxygenase 2
/
Molecular Docking Simulation
/
Analgesics
/
Imidazoles
Limits:
Animals
/
Humans
/
Male
Language:
En
Journal:
Future Med Chem
Year:
2024
Document type:
Article
Affiliation country: