RESUMEN

A number of new 3-aryl-1,2,3,4-oxatriazole-5-imine derivatives (GEA Compounds--GEAC) were synthetized. GEAC are NO-releasers as evidenced by direct measurement of NO in headspace/NO-analyzer, by cooxygenation of oxyhaemoglobin to methaemoglobin in the Werringloer's test and by generation of nitrite in the Griess' reaction. During the release of NO from GEAC the consumption of O2 could be detected only when high concentrations of GEAC were used. The mechanism of release of NO from molecules of GEAC still remains hypothetical. Some of GEAC were found to remain stable for long periods of time, even at 37 degrees C. Both mutagenic properties and the pharmacodynamic profile of GEAC can be controlled by a mindful choosing of appropriate substituents.

Asunto(s)

Óxido Nítrico/metabolismo , Oxadiazoles/síntesis química , Triazoles/síntesis química , Animales , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión , Semivida , Hemoglobinas/metabolismo , Espectroscopía de Resonancia Magnética , Masculino , Metahemoglobina/metabolismo , Pruebas de Mutagenicidad , Oxadiazoles/metabolismo , Oxadiazoles/farmacocinética , Oxadiazoles/farmacología , Oxidación-Reducción , Consumo de Oxígeno/efectos de los fármacos , Ratas , Ratas Sprague-Dawley , Estándares de Referencia , Espectrofotometría Infrarroja , Relación Estructura-Actividad , Triazoles/metabolismo , Triazoles/farmacocinética , Triazoles/farmacología