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J Enzyme Inhib Med Chem ; 38(1): 2162511, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36633257

RESUMO

A novel series of 12 antipyrine derivatives containing 1,3,4-oxadiazoles (4a-d), 1,3,4-thiadiazoles (6a-d), and pyrimidines (8a-d), was preparedand assessed for its potential in vitro COX-2 inhibitors. Compared to Celecoxib, compounds 4b-d and 8d were the most potent derivatives c with a half-maximal inhibitory concentration range of 53-69 nM. Considering COX-2 selectivity index, compounds 4 b and 4c were chosen among these most potent derivatives for further investigation. The in vivo ability of compounds 4 b and 4c to counteract carrageenan-induced paw edoema has been assessed and their potential underlying mechanisms have been elucidated and the results have been further validated using molecular docking simulations.


Assuntos
Anti-Inflamatórios , Antipirina , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Antipirina/farmacologia , Celecoxib/farmacologia , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Desenho de Fármacos , Edema/tratamento farmacológico , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
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