RESUMEN

Benzoylacetonitrile and beta-aminocinnamonitrile are shown to possess potent antiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogues, only o-, m-, and p-fluorobenzoylacetonitrile and m- and p-fluoro-beta-aminocinnamonitrile retained activity. Additionally, beta-amino-2- and beta-amino-3-thiopheneacrylonitrile and beta-oxo-2- and beta-oxo-3-thiophenepropionitrile exhibited similar activity. These agents are not believed to be acting via prostaglandin synthetase inhibition. The metabolic profile of benzoylacetonitrile is also described.

Asunto(s)

Acetonitrilos/síntesis química , Antiinflamatorios/síntesis química , Nitrilos/síntesis química , Acetonitrilos/metabolismo , Acetonitrilos/farmacología , Acetonitrilos/uso terapéutico , Animales , Artritis Experimental/tratamiento farmacológico , Edema/tratamiento farmacológico , Eritema/tratamiento farmacológico , Cobayas , Nitrilos/farmacología , Nitrilos/uso terapéutico , Ratas , Relación Estructura-Actividad