RESUMEN
Two novel series of pyrimidine derivatives have been prepared, namely; 3,6-disubstituted perhydropyrimidine-2,4-diones 8a-l as well as 3,6-disubstituted 2-thioxo-perhydropyrimidine-4-ones 9a-k. The anticancer as well antimicrobial activities of these compounds and their open-chain counterparts have been determined.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Pirimidinonas/síntesis química , Pirimidinonas/farmacología , Tionas/síntesis química , Tionas/farmacología , Antibacterianos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Indicadores y Reactivos , Pruebas de Sensibilidad Microbiana , Relación Estructura-Actividad , Células Tumorales CultivadasRESUMEN
Three main classes of quinoxaline derivatives have been synthesized. The first class comprises the synthesis of three novel series of 1,2,4-triazolo[4,3-a]quinoxalines; namely 1-substituted-1,2,4-triazolo[4,3-a]quinoxalines 3a-f, 1-substituted aminomethyl-1,2,4-triazolo[4,3-a]quinoxalines 14a-d and 1-cyano or ethoxycarbonylmethyl-1,2,4-triazolo[4,3-a]quinoxalines 6, 12. The second class involves the synthesis of 2-substituted-1 H-1,2,4-triazino[4,3-a]quinoxalines 4a-d. The third class deals with the synthesis of a variety of 2-pyrazolylquinoxalines, namely 2-(5-amino-3-arylpyrazol-1-yl)-3-phenylquinoxalines 5a-d, 2-[5-hydroxy-3-phenyl-4-(4-substituted sulfamoylphenyl)azopyrazol-1-yl]-3-phenylquinoxalines 15a, b, and 2-(5-hydroxy-4-nitroso-3-phenylpyrazol-1-yl)-3-phenylquinoxalin e (16). The prepared compounds were tested in vitro for their antimicrobial activity. Compounds 13 and 14b exhibited promising antifungal activity against C. albicans (MIC 25, 50 mu/ml respectively). Compound 13 was as active as the antibiotic nystatin.
Asunto(s)
Antiinfecciosos/síntesis química , Quinoxalinas/síntesis química , Antibacterianos , Antiinfecciosos/farmacología , Candida albicans/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Quinoxalinas/farmacología , Staphylococcus aureus/efectos de los fármacosRESUMEN
The bactericidal activity of 0.1% benzydamine (CAS 642-72-8, BD), a non-steroidal anti-inflammatory agent was evaluated by the viable count technique against 12 multifold resistant clinical isolates. An efficient rapid activity was obtained irrespective of the antibiotic resistance pattern. Combinations of 0.1% BD and ampicillin, chloramphenicol or tetracycline exerted synergistic bactericidal activity against antibiotic resistant Pseudomonas aeruginosa and Staphylococcus aureus isolates. Using the chessboard technique, out of 114 BD-antibiotic bacteriostatic combinations, 19 were partially synergistic and the remaining were indifferent. The effect of subinhibitory concentrations of BD-ampicillin, BD-chloramphenicol and BD-tetracycline on the growth of the test organisms revealed significant synergism, especially with tetracycline combinations, most likely due to enhanced uptake of the antibiotic by the organisms in the presence of BD.
Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Infecciones Bacterianas/microbiología , Bencidamina/farmacología , Bacterias/crecimiento & desarrollo , Combinación de Medicamentos , Resistencia a Múltiples Medicamentos , Sinergismo Farmacológico , Humanos , Pruebas de Sensibilidad MicrobianaRESUMEN
The antimicrobial activity of benzydamine (BD), a non-steroid anti-inflammatory agent, was studied using different techniques against 38 strains belonging to 12 microbial species comprising bacteria, yeasts and a fungus. The minimum inhibitory concentrations, minimum lethal concentrations, per cent survivors after 30-minute exposure to BD (0.1%), growth curves of 7 selected organisms in subinhibitory BD concentrations and killing times for clinical isolates at different BD levels (0.05-0.15%) were determined. The data obtained throughout this study show that BD is a general antimicrobial agent with a rapid biocidal activity against a variety of organisms at concentrations less than those advocated for treatment of inflammatory conditions.
Asunto(s)
Antiinfecciosos/farmacología , Bencidamina/farmacología , Antibacterianos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Gramnegativas/crecimiento & desarrollo , Bacterias Grampositivas/efectos de los fármacos , Bacterias Grampositivas/crecimiento & desarrollo , Pruebas de Sensibilidad Microbiana , Especificidad de la Especie , Factores de Tiempo , Levaduras/efectos de los fármacos , Levaduras/crecimiento & desarrolloRESUMEN
A simple and precise agar diffusion microassay was developed for rifampicin (RIF) in serum. The method involved the addition of sera containing RIF (0.125-4.0 micrograms/ml) to wells cut in an agar medium (pH 6.6) surface seeded with an adjusted inoculum of Staphylococcus aureus ATCC 6538 P and incubated for 2h at 40 degrees C. Repetitive assays of sera containing known concentrations of RIF revealed an average mean recovery of 93.6% with a coefficient of variation of 5.7%. This rapid method allowed accurate determination of RIF in the presence of erythromycin, chloramphenicol, lincomycin and amikacin. These four antibiotics were also separately measured in sera by the rapid assay at different pH values.