Synthesis and antituberculosis action of some new pyruvic acid derivatives.

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.

Researches concerning the synthesis and antituberculosis action of some new sulphacetamide derivatives.

In the present study we emphasized the antituberculosis action of new sulphacetamide derivatives. In order o extend the research for obtaining antituberculosis substances, we decided to study the influence of the introducing of the thiourea and sulphamide groups in the molecule on the antituberculosis activity of the Isoniazid. We have developed a simple and precise method for obtaining the thiourea derivatives of sulphamides' isonicotinoilhydrazone. The structure of the newly synthesized compounds was confirmed by the quantitative elemental analysis as well as IR spectral measurements. We tested the antituberculosis action of new eight obtained sulphacetamide derivatives. Testing new substances on the Mycobacterium tuberculosis complex implies the insemination of inoculums on tubes containing the new substances, in chosen concentrations. Early tests on Mycobacterium tuberculosis strains show susceptibility to these new compounds (for the tested concentrations). The new compounds represent a premise for obtaining new antimycobacterial agents.

[New methyl-quinoxaline derivatives with antimicrobial activity]. / Nouveaux derivés de la 6-méthyle-quinoxaline doués d'activité antimicrobienne.

This paper presents the synthesis of six new quinoxaline derivatives cycloadditions products of N-monoxide and N,N'-dioxide of 6-methyl-quinoxaline. The chemical structure of new azabicyclic products was confirmed by C, H, N elemental analysis and spectral analysis (IR and RMN). We have tested the antimicrobial activity of the new synthesized azabicyclic derivatives by the diffusimetric method. The assay was made on the seven microorganisms, gram-positive and gram-negative bacteria. The results show that the new compounds are more active against the gram-positive bacteria and Candida albicans.