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Rev Med Chir Soc Med Nat Iasi ; 112(3): 860-4, 2008.
Artículo en Inglés | MEDLINE | ID: mdl-20201282

RESUMEN

UNLABELLED: The present paper studies the synthesis and activity of 12 new azoic derivatives against Mycobacterium tuberculosis. MATERIAL AND METHOD: In order to obtain new antituberculosis substances, we studied 6 thiadiazolic derivatives and 6 triazolic derivatives of pyruvic acid and we observed the influence of the different radical groups inserted in the molecule on their antituberculosis activity. For this study we developed a simple method to obtain the new derivatives. The first stage of the experiment was the synthesis of the thyosemicarbazide derivatives. In order to obtain the thiadiazolic derivatives we treated the thyosemicarbazides with concentrated sulfuric acid. The triazolic derivatives were obtained after treating the thiosemicarbazide derivatives with a diluted NaOH solution at boiling. RESULTS: The structure of the substances was furthermore confirmed by IR and quantitative elemental analysis. The newly obtained substances were tested on the Mycobacterium tuberculosis complex, 6 concentrations for each substance. Early tests on Mycobacterium tuberculosis indicate that 2 of the tested substances have clear antituberculosis activity in vitro for the tested concentrations. For the other tested substances further research is needed since the CMI hasn't been reached in their cas. CONCLUSIONS: We synthesised 12 new thiadiazolic and triazolic derivatives in order to obtain new possible antituberculosis agents. Early tests on Mycobacterium tuberculosis indicate that 2 of the tested substances have clear antituberculosis activity in vitro for the tested concentrations.


Asunto(s)
Antituberculosos/síntesis química , Antituberculosos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Ácido Pirúvico/síntesis química , Ácido Pirúvico/farmacología , Tiadiazoles/síntesis química , Tiadiazoles/farmacología , Antituberculosos/química , Inhibidores Enzimáticos/síntesis química , Humanos , Técnicas In Vitro , Pruebas de Sensibilidad Microbiana , Ácido Pirúvico/química , Semicarbacidas/síntesis química , Hidróxido de Sodio/química , Ácidos Sulfúricos/química , Tiadiazoles/química , Triazoles/síntesis química , Tuberculosis/tratamiento farmacológico , Tuberculosis/microbiología
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