RESUMO
A group of seven acidic phenyl derivatives of some fused imidazole systems were subjected to a series of tests in vivo in order to evaluate their pharmacological activity. Antiinflammatory activity was studied by means of the carrageenin-induced rat paw edema. Hot plate test and writhing induced by acetic acid in mice were used to evaluate analgesic activity. Yeast-induced hyperthermia in rats was employed to study antipyretic action. Irritative and ulcerogenic action on the rat gastric mucosa was examined at higher doses. The antiaggregating activity and the inhibition of platelet malondialdehyde production were studied in vitro. All experimental results are discussed from the point of view of structure-activity relationships and mode of action.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Imidazóis/farmacologia , Animais , Plaquetas/efeitos dos fármacos , Plaquetas/metabolismo , Feminino , Cavalos , Técnicas In Vitro , Masculino , Malondialdeído/sangue , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação Plaquetária , Gravidez , Ratos , Tempo de Reação/efeitos dos fármacos , Úlcera Gástrica/induzido quimicamenteRESUMO
The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.
