N-(β- d -甘氨酰基)-硫代氨基脲的合成、生物活性及毒性评价

B. Ernazarova, A. Dzhumanazarova, Aida Bakirova, Z. Abdullaeva, G. Zhusupbaeva, Zarylkan Asylbek Kyzy, M. Arzybaev
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引用次数: 2

摘要

在现代科学中,优先考虑的是寻找具有特殊性质的生物活性化合物。通过实验数据发现,N-(β- d -甘氨酰基)-氨基脲与Lawesson试剂(2,4-二(对甲氧基苯基)-1,3-二硫代二硫烷)在吡啶中以1:1的比例反应,在水浴回流煮沸20 ~ 35分钟后,生成了新的合成化合物N-(β- d -甘氨酰基)-氨基脲。通过13C NMR、1H NMR、IR和元素分析对目标产物的个性和结构进行了证实。对合成的N-(β- d -甘氨酰基)-硫代氨基脲新化合物,用计算机方法预测了其药理作用和毒性作用的概率。从合成的化合物N-(β-D-galactopyranosyl)-硫代氨基脲预测其抗菌(抗菌)活性概率(Pa/Pi 0.544/0.013)。该化合物(4)的抗菌活性在对羔羊沙门氏菌感染、小牛沙门氏菌病和大肠杆菌血清型的试验中得到证实。体外实验研究表明,新合成的化合物N-(β- d -半乳糖酰基)-硫代氨基脲在所研究浓度下具有明显的杀菌抑菌作用。合成的新化合物N-(β- d -糖基-吡喃基)-硫代氨基脲是一个值得进一步研究的化合物。
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Synthesis, Assessment of Biological Activity and Toxicity for N-(β-D-Glycopyranosyl)-Thiosemicarbazides
In the modern science, priority is given for the search of biological active compounds with specific properties. As a result of experimental data, it was found that in the reaction between N-(β-D-glycopyranosyl)-semicarbazide and the Lawesson reagent (2,4-bis(p-methoxyphenyl)-1,3-dithiadiphosphetane 2,4-disulfide) at the ratio 1:1 in pyridine when boiling under reflux in a water bath for 20 - 35 minutes, a new synthetic compound N-(β-D-glycopyranosyl)-thiosemicarbazide is formed. The individuality and structure of the target products were confirmed by 13C NMR spectroscopy, 1H NMR spectroscopy, IR spectroscopy, and elemental analysis. For the synthesized new compounds of N-(β-D-glycopyranosyl)-thiosemicarbazides, the probability of pharmacological and toxic effects were predicted by the computer method in silico. From the synthesized compounds N-(β-D-galactopyranosyl)-thiosemicarbazide, the probability of antibacterial (antibacterial) activity is predicted (Pa/Pi 0.544/0.013). The antibacterial activity of the compound (4) was confirmed in a test for salmonella infection of lambs, salmonellosis of calves, and colipathogenic E. coli serotypes. An experimental study by the in vitro method made it possible to conclude that the new synthetic compound N-(β-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effect. The synthetic new compound N-(β-D-glyco- pyranosyl)-thiosemicarbazide is a promising compound for further study.
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