RESUMO
A new series of 2-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazole derivatives containing a 1,2,4-triazole ring were synthesized via microwave technique. This efficient procedure provides pure products within a few minutes. The newly synthesized compounds were confirmed by (1) H NMR and (13) C NMR spectra and they were screened for their lipase inhibition and antioxidant activities. Compounds 4a, 4b, 5a, and 5b showed very good scavenging activity.
Assuntos
Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/farmacologia , Lipase/antagonistas & inibidores , Micro-Ondas , Triazóis/síntese química , Triazóis/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Lipase/metabolismo , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Picratos/química , Relação Estrutura-Atividade , Ácidos Sulfônicos/químicaRESUMO
Some novel 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazol-3-one (3, 6, 8, 9) derivatives and or 3-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3]benzoxazole (5) were synthesized from the reaction of various ester ethoxycarbonylhydrazones (1a-e) with several primary amines. The synthesis of 4-amino-5-(4-chlorophenyl)-2-[(5-mercapto-1,3,4-oxadiazol-2-yl)methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one (13) was performed starting from 4-Amino-5-(4-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (2) by four steps; then 13 was converted to the corresponding Schiff base (14) by using 4-methoxybenzaldehyde. Finally, two Mannich base derivatives of 14 were obtained by using morpholine or methyl piperazine as amine component. All newly synthesized compounds were screened for their antimicrobial activities and some of which were found to possess good or moderate activities against the test microorganisms.
