Synthesis and antituberculosis action of some new pyruvic acid derivatives.
The present paper studies the synthesis and activity of 12 new azoic derivatives against Mycobacterium tuberculosis.


METHODS
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.
Ungureanu
Margareta
M
Scholl of Medical Bioengineering, "Gr.T. Popa" University of Medicine and Pharmacy Iaşi.
Diculencu
Daniela
D
Archip
Cristina
C
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D006801:Humans; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D019289:Pyruvic Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012663:Semicarbazides / Q000138:chemical synthesis; D012972:Sodium Hydroxide / Q000737:chemistry; D013464:Sulfuric Acids / Q000737:chemistry; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis; D014376:Tuberculosis / Q000188:drug therapy / Q000382:microbiology
D000995:Antitubercular Agents; D004791:Enzyme Inhibitors; D012663:Semicarbazides; D013464:Sulfuric Acids; D013830:Thiadiazoles; D014230:Triazoles; D012972:Sodium Hydroxide; C005151:thiosemicarbazide; D019289:Pyruvic Acid; C033158:sulfuric acid