RESUMEN
The generation and reactivity of 3-triazolyl-nitrosoalkenes are reported for the first time. The study showed that hetero-Diels-Alder reaction of these heterodienes is an interesting synthetic strategy to functionalized 1,2,3-triazoles, including 1,2,3-triazolyl-pyrroles, 1,2,3-triazolyl-dipyrromethanes and 1,2,3-triazolyl-indoles. The evaluation of the antibacterial profile against Gram-positive and Gram-negative strains revealed the new 5,5'-diethyldipyrromethane bearing a side chain incorporating a triazole and oxime moieties. The antibacterial profile detected was within the Clinical and Laboratory Standard Institute (CLSI) range and against important Staphylococcus species including Methicillin-resistant strain (S. aureus ATCC 25923, S. epidermidis ATCC 12228 and S. simulans ATCC 27851 and MRSA). Interestingly, this new 1,2,3-triazole presented hemocompatibility and low in silico toxicity profile similar to antibiotics current in use. It also has an usual antibiofilm activity against MRSA, which reinforced its potential as a new antibacterial prototype.
Asunto(s)
Antibacterianos/farmacología , Staphylococcus/efectos de los fármacos , Triazoles/farmacología , Alquenos/química , Antibacterianos/síntesis química , Antibacterianos/química , Biopelículas/efectos de los fármacos , Reacción de Cicloadición , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Compuestos Nitrosos/química , Staphylococcus/crecimiento & desarrollo , Relación Estructura-Actividad , Triazoles/síntesis química , Triazoles/químicaRESUMEN
The protein p53 is considered to be one of the most important tumor suppressor factors. Despite this importance, a potential association between TP53 messenger (m)RNA levels and tumor aggressiveness has not been well defined in animal cancer. We assessed and correlated TP53 gene expression in 40 canine mammary carcinomas with histologic grade, tumor size, and aggressiveness. The tumors were subjected to histologic analysis and the TP53 mRNA levels determined by RT-rtPCR. Statistical analysis revealed no correlation between levels of TP53 mRNA and tumor aggressiveness ( r = 0.00) or tumor growth ( r = 0.06). Histologic grades ( r = 0.17) and mitosis count ( r = 0.12) showed a weak correlation with TP53 mRNA expression levels. These findings are consistent with molecular studies that revealed heterogeneous expression of TP53 in canine and human mammary tumors. Hence, TP53 gene expression alone cannot be considered a marker for tumor aggressiveness in canine mammary carcinomas.
