Design, synthesis, characterization and in vitro and in vivo anti-inflammatory evaluation of novel pyrazole-based chalcones.
J Enzyme Inhib Med Chem
; 30(1): 22-31, 2015 Feb.
Article
em En
| MEDLINE
| ID: mdl-24666306
ABSTRACT
Abstract A series of novel pyrazole-based chalcones have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxyphenyl)-1H-pyrazole (6). The structures of regioisomers 6 and 7 were determined by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds were tested for their inhibitory activity against COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model for acute inflammation and cotton pellet-induced granuloma model for chronic inflammation. All the synthesized compounds showed potential to demonstrate anti-inflammatory activities, of particular interest compounds 10i, 10e, 10f, and 10h were found to be potent anti-inflammatory agents.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Pirazóis
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Anti-Inflamatórios não Esteroides
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Inibidores de Ciclo-Oxigenase
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Chalconas
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Edema
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Granuloma
Limite:
Animals
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article