RESUMO
1-(2-Adamantyl-3-(5-arylhydrazono-6-methyl-4-oxopyrimidin -2-yl)guanidines, 2-(2-adamantylamino)-4-amino-s-triazine and its 6-chloromethyl derivative were prepared by cyclization of 1-(2-adamantyl)biguanide.HCl with ethyl 2-arylhydrazono-3-oxobutyrates, ethyl formate and ethyl chloroacetate, respectively. 1-(2-damantyl)-3-(4,5-dioxo-2-imidazolidinylidene)guanidine was used as intermediate for the synthesis of amides, hydrazide and azomethine derivatives of alkyl 2-(2-adamantylamino)-4-amino-s-triazine-6-carboxylates. The antimicrobial testing of the prepared compounds proved that an azomethine derivative was the most active. It showed a marked bacteriostatic effect against Staphylococcus aureus and Bacillus subtilis.
Assuntos
Adamantano/análogos & derivados , Antibacterianos/síntese química , Bactérias/efeitos dos fármacos , Guanidinas/síntese química , Triazinas/síntese química , Adamantano/síntese química , Adamantano/farmacologia , Bacillus subtilis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Guanidinas/farmacologia , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos , Triazinas/farmacologiaRESUMO
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
3-(3 or 4-Acetylphenyl)-sydnones 7, 8 have been synthesized by formation of the glycines 3, 4, followed by nitrosation to 5, 6 and cyclization with acetic anhydride to sydnones. Sydnone derivatives carrying chalcone moieties 15, 16 were prepared by formation of the chalcone analogues 11, 12 through condensation of the glycines 3, 4 with the appropriate aldehydes, followed by the reactions applied for the preparation of 7, 8. The sydnone derivatives were screened for antimicrobial activities.