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1.
Bioorg Med Chem ; 20(13): 4149-54, 2012 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-22633120

RESUMEN

Structurally modified phthalimide derivatives were prepared through condensation of phthalic and tetrafluorophthalic anhydride with selected sulfonamides with variable yields. All compounds were screened for their antimycobacterium activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) using a micro broth dilution technique. The fluorinated derivatives (compounds 2c, 2d, 2f and 2h) had antimycobacterium activity comparable with classical sulfonamide drugs. The minimum inhibitory concentration (MIC) of compounds 2c, 2d, 2f and 2h was greater than that of isoniazid (MIC<0.02 µg/mL) and in vitro activity was greater than that of pyrazinamide, another first line antimycobacterium drug (MIC 50-100 µg/mL). The new compounds could be considered new lead compounds in the treatment of multi-drug resistant tuberculosis.


Asunto(s)
Antituberculosos/síntesis química , Ftalimidas/química , Animales , Antituberculosos/farmacología , Antituberculosos/toxicidad , Línea Celular , Supervivencia Celular/efectos de los fármacos , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Isoniazida/farmacología , Ratones , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos , Ftalimidas/farmacología , Ftalimidas/toxicidad , Pirazinamida/farmacología
2.
Diagn Microbiol Infect Dis ; 72(4): 350-7, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22277535

RESUMEN

We have evaluated the efficiency of the TK Rapid Mycobacterial Culture System in isolating mycobacteria from clinical samples and in susceptibility testing. The TK Medium indicates mycobacterial growth by changing its color from red to yellow. During a 1-year period, 16,303 clinical samples were inoculated to TK selective (TK SLC) and Löwenstein-Jensen media (LJ). Mycobacteria were isolated in 2150 (13.04%) samples in at least 1 type of medium. While LJ isolated mycobacteria from 1920 (11.69%) of all samples, TK SLC isolated 2070 (12.63%). Among all positives, the isolation rates for LJ and TK SLC were 89.30% and 96.27%, respectively. Contamination of cultures by other organisms was observed in 878 (5.33%) LJ tubes and in 90 (0.55%) TK SLC tubes. On average, time-to-growth detection was 15.57 days in TK SLC and 25.14 days in LJ. The modes of time-to-growth detection were 12 and 25 days for TK SLC and LJ, respectively. The reliability of antimycobacterial susceptibility testing was checked by 36 Mycobacterium tuberculosis strains with known susceptibility patterns which were obtained from the World Health Organization collection and by participating in an external quality control program. All susceptibility results, except for a few borderline-resistant strains, were consistent with the expected susceptibility patterns. The TK Rapid Mycobacterial Culture System is a practical and reliable automated system that shortens the time required for both culture and susceptibility results. All types of TK Media are ready to use, saving time and effort as well as drastically reducing contamination during testing.


Asunto(s)
Antituberculosos/farmacología , Técnicas Bacteriológicas/métodos , Medios de Cultivo/química , Mycobacterium tuberculosis/efectos de los fármacos , Mycobacterium tuberculosis/crecimiento & desarrollo , Tuberculosis/diagnóstico , Automatización , Humanos , Pruebas de Sensibilidad Microbiana/métodos , Mycobacterium tuberculosis/aislamiento & purificación , Reproducibilidad de los Resultados , Esputo/microbiología , Factores de Tiempo , Tuberculosis/microbiología
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