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Chemotherapy ; 61(5): 249-55, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26950478

RESUMO

New compounds with antituberculosis activity and their combination with classic drugs have been evaluated to determine possible interactions and antagonism. The aim of this study was to evaluate the in vitro activity of Casiopeínas® copper-based compounds (CasIIIia, CasIIIEa, and CasIIgly) alone and combined with isoniazid (INH), rifampicin, or ethambutol (EMB) against resistant and susceptible Mycobacterium tuberculosis. Seventeen clinical M. tuberculosis isolates (5 multi-drug resistant and 2 resistant to INH and/or EMB) were subjected to determination of the minimal inhibitory concentration (MIC) by the resazurin microtiter assay and combination assessment by the resazurin drug combination microtiter assay. The Casiopeínas® alone showed a remarkable effect against resistant isolates with MIC values from 0.78 to 12.50 µg/ml. Furthermore, a synergistic effect mainly with EMB is shown for both resistant and susceptible clinical isolates. Casiopeínas® are promising candidates for future investigation into the development of antituberculosis drugs, being one of the first examples of essential metal-based drugs used in this field.


Assuntos
Antituberculosos/farmacologia , Complexos de Coordenação/farmacologia , Cobre/química , Mycobacterium tuberculosis/efeitos dos fármacos , Tuberculose/microbiologia , Antituberculosos/química , Antituberculosos/uso terapêutico , Complexos de Coordenação/química , Complexos de Coordenação/uso terapêutico , Farmacorresistência Bacteriana/efeitos dos fármacos , Sinergismo Farmacológico , Etambutol/farmacologia , Etambutol/uso terapêutico , Humanos , Isoniazida/farmacologia , Isoniazida/uso terapêutico , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/microbiologia , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/isolamento & purificação , Rifampina/farmacologia , Rifampina/uso terapêutico , Tuberculose/tratamento farmacológico
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