RESUMO
Certain derivatives of quinazoline and its bioisostere pyridopyrimidine carrying important structural features that contribute to diuretic activity, such as sulfonamido, morpholino and chlorophenyl, were prepared as potential diuretic agents. Likewise, some tricyclic 1,2,4-triazolo[3,4-b]quinazolines and pyrido[3,2-d][1,2,4]triazolo[4,3-alpha] pyrimidines with the same features were reported. Nine compounds were tested for the diuretic activity in rats and the results showed that the active compound is 7-chloro-2-methyl-3-phthalimido-4(3H)-quinazoline (4).
Assuntos
Diuréticos/síntese química , Pirimidinas/síntese química , Animais , Diuréticos/farmacologia , Diuréticos/toxicidade , Feminino , Masculino , Pirimidinas/farmacologia , Pirimidinas/toxicidade , RatosRESUMO
Condensation of 2-methyl-6-nitro-4-quinazolone with different aldehydes was achieved by fusing the reactants in the presence of zinc chloride, affording 2-substituted styryl-6-nitro-4-quinazolones. 2-(3-substituted aminomethyl)-4-hydroxystyryl-6-nitro-4-quinazolones were also prepared through the Mannich reaction. The antimicrobial testing of five of the compounds prepared showed that some of them produce promising effects.
