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Eur J Med Chem ; 44(1): 117-23, 2009 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-18455273

RESUMO

The present investigation is concerned with the synthesis of different acylated 1,2,4-triazole-3-acetates with the objective of discovering novel and potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by spectral and elemental analyses. The obtained compounds were evaluated for their anti-inflammatory activites as well as gastric ulcerogenic effects and acute toxicity. Results showed that 1-acylated-5-amino-1,2,4-triazole-3-acetates 3a-e showed higher anti-inflammatory activity than the corresponding 5-acylamino derivatives 4a-e in carageenan-induced rat paw edema test with low gastric ulcerogenicity compared with indomethacin. Furthermore, molecular modeling studies were performed in order to rationalize the obtained biological results.


Assuntos
Acetatos/síntese química , Anti-Inflamatórios/síntese química , Desenho de Fármacos , Triazóis/síntese química , Acetatos/farmacologia , Acetatos/uso terapêutico , Acilação , Animais , Anti-Inflamatórios/farmacologia , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Edema/tratamento farmacológico , Edema/prevenção & controle , Modelos Moleculares , Estrutura Molecular , Ratos , Úlcera Gástrica/tratamento farmacológico , Triazóis/farmacologia , Triazóis/uso terapêutico
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