Asunto(s)
Guanidinas , Hipoglucemiantes , Animales , Glucemia/metabolismo , Carbamatos/síntesis química , Carbamatos/farmacología , Ésteres , Guanidinas/síntesis química , Guanidinas/farmacología , Hipoglucemiantes/síntesis química , Hipoglucemiantes/farmacología , Masculino , Métodos , Conejos , RatasAsunto(s)
Antiinflamatorios/síntesis química , Hidantoínas/síntesis química , Uracilo/síntesis química , Animales , Antiinflamatorios/uso terapéutico , Fenómenos Químicos , Química , Hidantoínas/uso terapéutico , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Caolín , Ratas , Uracilo/uso terapéuticoRESUMEN
Two series of compounds, 2,3-dihydro-9H-isoxazolo[3,2-b]quinazolin-9-ones and 3,4-dihydro-(1,2)-oxazino-[3,2-b]quinazolin-10(2H)-ones, were synthesized and evaluated for anti-inflammatory, antipyretic and analgesic activity. The isoxazolo compounds were generally more active than their oxazino homologs. Three compounds, i.e., 2,3-dihydro-9H-isoxazolo [3,2-b]quinazolin-9-one (W-2429) and its 2- and 3-methyl congeners, were the most active of all compounds tested in this study. On the basis of the biological results herein reported, W-2429 is considerably more effective than acetylsalicylic acid in inhibiting carrageenan-induced edema and in reducing brewer's yeast-induced fever in rats. Also, it was found to be more potent than propoxyphene hydrochloride in the Randall-Selitto test for analgesic activity.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Quinazolinas/síntesis química , Animales , Isoxazoles/síntesis química , Isoxazoles/farmacología , Oxazinas/síntesis química , Oxazinas/farmacología , Quinazolinas/farmacología , Ratas , Relación Estructura-ActividadRESUMEN
p-Chlorophenylthiobutanol (W-2719) has been found to effectively inhibit immunologic and non-immunologic histamine release and mast cell degranulation. It has been found to effectively suppress passive cutaneous anaphylaxis (PCA) reaction not be antihistaminic action, but by inhibiting the release of allergic mediators.
Asunto(s)
Butanoles/farmacología , Hipersensibilidad Inmediata/prevención & control , Animales , Cobayas , Liberación de Histamina/efectos de los fármacos , Leucocitos/ultraestructura , Pulmón/efectos de los fármacos , Masculino , Mastocitos/efectos de los fármacos , Anafilaxis Cutánea Pasiva/efectos de los fármacos , Conejos , RatasRESUMEN
A series of 3,3a-dihydro-2H,9H-isoxazolo[3,2-b]-[1,3]benzoxazin-9-ones was synthesized and evaluated for anti-inflammatory, antipyretic and analgesic activity. Since many of these compounds exhibited promising activity, particularly in the anti-inflammatory tests, a number of homologous 2,3,4,4a-tetrahydro-10H-1,2-oxazino[3,2-b]-[1,3]benzoxazin-10-ones and one 3,4,5,5a-tetrahydro-2H, 11H,-1,2-oxazepino [3,2-b][1,3]benzoxazin-11-one, the 9-chloro analog, were also prepared and evaluated. The expanded ring members were generally less active than the tricyclic compounds containing the isoxazolidine ring.