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Synthesis, assessment of biological activity and Toxicity for N-(<i>β</i>-D-Glycopyranosyl)-Thiosemicarbazides

International Journal of Organic Chemistry 2020年第4期10卷 159-169页

作者： Baktygul Ernazarova Asylkan Dzhumanazarova Aida Bakirova Zhypargul Abdullaeva Gulsara Zhusupbaeva Zarylkan Asylbek Kyzy Momun Arzybaev Department of Medical-biological Disciplines Zhalal-Abad State University Zhalal-Abad Kyrgyzstan Institute of Chemistry and Phytotechnology National Academy of Sciences Bishkek Kyrgyzstan Science and Research Department Osh State University Jolon Mamytov Campus Osh Kyrgyzstan Zhalal-Abad Scientific Center South Department Academy of Sciences Zhalal-Abad Kyrgyzstan Department of Pharmacy and Medical-biological Disciplines Zhalal-Abad State University Zhalal-Abad Kyrgyzstan Department of Biotechnology Kyrgyz National Agrarian University Named after K.I. Skryabin Bishkek Kyrgyzstan

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.

关键词： assessment of biological activity Synthesis of Carbohydrate Derivatives of Urea Toxicity Antibacterial Antiviral activity

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