Ungureanu Margareta, Diculencu Daniela, Archip Cristina
Scholl of Medical Bioengineering, "Gr.T. Popa" University of Medicine and Pharmacy Iaşi.
Rev Med Chir Soc Med Nat Iasi. 2008 Jul-Sep;112(3):860-4.
The present paper studies the synthesis and activity of 12 new azoic derivatives against Mycobacterium tuberculosis.
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.
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.
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.
本文研究了12种新型偶氮衍生物对结核分枝杆菌的合成及活性。
为了获得新型抗结核物质，我们研究了丙酮酸的6种噻二唑衍生物和6种三唑衍生物，并观察了分子中插入的不同基团对其抗结核活性的影响。为进行此项研究，我们开发了一种简单方法来获得新型衍生物。实验的第一阶段是合成硫代氨基脲衍生物。为了获得噻二唑衍生物，我们用浓硫酸处理硫代氨基脲。用稀释的氢氧化钠溶液在沸腾条件下处理硫代氨基脲衍生物后得到三唑衍生物。
通过红外光谱和定量元素分析进一步证实了这些物质的结构。对新获得的物质在结核分枝杆菌复合体上进行了测试，每种物质设6个浓度。对结核分枝杆菌的早期测试表明，在所测试的浓度下，有2种受试物质在体外具有明确的抗结核活性。对于其他受试物质，由于尚未达到临界最小抑菌浓度，因此需要进一步研究。
我们合成了12种新型噻二唑和三唑衍生物，以获得新型潜在抗结核药物。对结核分枝杆菌的早期测试表明，在所测试的浓度下，有2种受试物质在体外具有明确的抗结核活性。
