RESUMEN
Synthesis of a series of 7-arylidene-6-(2,4-dichlorophenyl)-3-aryloxymethyl/anilinomethyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (3) by the condensation of 3-aryl-1-(2,4-dichloro-5-fluorophenyl)-2-bromo-propen-1-one (1) and 4-amino-5-mercapto-3-aryloxymethyl/anilinomethyl-1,2,4-triazoles (2) is described. The newly synthesized compounds were characterized by elemental analysis IR, 1H NMR and mass spectral data. These compounds were tested for their antimicrobial activities against Escherichia coli, Staphylococcus aureus (Smith), Psuedomonas aeruginosa (Gessard), Bacillus subtilis and Candida albicans. Some of the newly synthesized compounds were also screened for their anticancer activity. Among them compounds 3m, 3o, 3q showed in vitro anticancer activity.
Asunto(s)
Antibacterianos/síntesis química , Antifúngicos/síntesis química , Antineoplásicos/síntesis química , Compuestos Azo/síntesis química , Compuestos Azo/farmacología , Flúor/química , Compuestos de Sulfhidrilo/química , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Compuestos Azo/química , Línea Celular Tumoral , Evaluación Preclínica de Medicamentos , Humanos , Estructura Molecular , Relación Estructura-ActividadRESUMEN
A series of 3-substituted 4-[5-(4-methoxy-2-nitrophenyl)-2-furfurylidene] amino-5-mercapto-1,2,4-triazoles (3) were synthesized. Aminomethylation of compounds 3 with formaldehyde and various secondary amines furnished Mannich bases 4 and 5. These compounds were characterized on the basis of IR, 1H-NMR, mass spectral data and elemental analysis. The newly synthesized compounds were screened for their anticancer activity against a panel of 60 cell lines derived from seven cancer types namely, lung, colon, melanoma, renal, ovarian, CNS and leukemia. Some of the compounds were slightly more potent.
Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Línea Celular Tumoral/efectos de los fármacos , Bases de Mannich/farmacología , Triazoles/química , Ensayos de Selección de Medicamentos Antitumorales , Furanos/química , Humanos , Espectroscopía de Resonancia Magnética , Bases de Mannich/síntesis química , Espectrometría de Masas , Espectrofotometría InfrarrojaRESUMEN
A number of N1 - arylfurfurylidene isatin -beta- hydrazones were prepared as possible antibacterial agents. They were subjected to Mannich reaction in the presence of secondary amines. The hydrazones and their Mannich bases were screened for their antibacterial properties against both Gram-negative bacteria.