Synthesis and biological evaluations of new nitric oxide-anti-inflammatory drug hybrids.
Bioorg Med Chem Lett
; 27(18): 4358-4369, 2017 09 15.
Article
em En
| MEDLINE
| ID: mdl-28844389
ABSTRACT
Three novel series of nitroso derivatives (11-15), isoxazolopyrazoles (17a-c) and isoxazolo[3,4-d]pyridazines (18a-c) were prepared from the hydroxyimoyl chloride 10. In vitro COX1⧹2 inhibition activities were evaluated, both of 17b and 18a proved a promising inhibitory activity with IC50=1.12, 0.78µM in sequent. Carrageenan induced Paw edema, ulcer liability, nitric oxide (NO) release and histopathological study were determined. Most of the prepared compounds showed excellent activities. Reactions of 2-aminopyridine and enaminone with hydroxyimoyl chloride 10 were investigated and proved by 2D NMR. Molecular docking for most active compounds was operated giving a hint for compound-receptor interactions.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Úlcera
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Anti-Inflamatórios não Esteroides
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Edema
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Óxido Nítrico
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2017
Tipo de documento:
Article