RESUMEN
The synthesis of 3-substituted 2-phenyl-2,3-dihydro-4H-1,3,2-benzoxazaphosphorin-4-one 2-sulfide derivatives is described. The action of a series 2-oxide (1-6) and 2-sulfide (7-12) derivatives on the central nervous system has been evaluated. Compounds 1-4, 6, 7-10 exhibit neuroleptic activity. Derivatives of sulfide series act as antiserotoninergic drugs.
Asunto(s)
Sistema Nervioso Central/efectos de los fármacos , Compuestos Organofosforados/síntesis química , Compuestos Organofosforados/farmacología , Animales , Antipsicóticos/síntesis química , Antipsicóticos/farmacología , Conducta Animal/efectos de los fármacos , Femenino , Masculino , Ratones , Ratas , Ratas Wistar , Antagonistas de la Serotonina/síntesis química , Antagonistas de la Serotonina/farmacología , Relación Estructura-ActividadRESUMEN
As a result of the reaction of salicylic amide with PCl3 and POCl3 2-chloro-2,3-dihydro-1,3,2-benzoxazaphosphorin-4-one (1) and its 2-oxide 2 are obtained. Compounds 1 and 2 form amides with amines in 2-position. Antineoplastic action of the derivatives containing the bis(2-chloroethyl)amide group in 2-position was found.
Asunto(s)
Antineoplásicos/síntesis química , Compuestos Organofosforados/síntesis química , Animales , Antineoplásicos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Leucemia L1210/tratamiento farmacológico , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Ratones Endogámicos DBA , Ratones Endogámicos , Compuestos Organofosforados/farmacología , Espectrofotometría InfrarrojaRESUMEN
A series of N-derivatives of 2-phenyl-2,3-dihydro-1,3,2(lambda 5)- benzoxazaphosphoryl-4-one and 2-phenyl-10-methyl-3a-triethoxyphosphonio- 1H,2,3,9,10-tetrahydropyrrolo[3,4-b]([1,4]benzoxazepine-1,3,9-trio ne have been prepared. The pharmacological investigation of the above mentioned compounds shows antitumor action against leukaemia in the case of three N-derivatives.
Asunto(s)
Leucemia L1210/tratamiento farmacológico , Compuestos Organofosforados/farmacología , Oxazepinas/farmacología , Animales , Femenino , Dosificación Letal Mediana , Ratones , Ratones Endogámicos DBA , Compuestos Organofosforados/síntesis química , Oxazepinas/síntesis químicaRESUMEN
Preparation of 2,3-dihydro-1,3,2-benzoxazaphosphorin-4-one derivatives and their 2-oxo derivatives is described. Compounds 1 and 12 have anticancer activity.