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Study of Biological Activity and Toxicity of Thiosemicarbazides Carbohydrate Derivatives by in Silico, in Vitro and in Vivo Methods

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Journal of Agricultural Chemistry and Environment 2022年第1期11卷 15-23页

作者： Baktygul Ernazarova Taitokur Zhusubaliev zarylkan asilbek kyzy Aida Bakirova Gulsara Zhusupbaeva Orozby Akparalieva Zhypargul Abdullaeva Nasibakhon Razykova Asilkan Dzhumanazarova Galina Apryshko Alina Orozmatova Department of Pharmacy and Medical-Biological Disciplines Zhalal-Abad State University Zhalal-Abad Kyrgyzstan Zhalal-Abad Scientific Center South Department Academy of Sciences Zhalal-Abad Kyrgyzstan Science and Research Department Osh State University Osh Kyrgyzstan Institute of Chemistry and Phytotechnology National Academy of Sciences Bishkek Kyrgyzstan National Medical Research Center of Oncology Named after N.N. Blokhin Moscow Russia

Computer analysis of N-(β-D-galactopyranosyl)-thiosemicarbazide compounds by in silico method revealed high probability of antibacterial (antimycobacterial), anti-tuberculosis (antituberculosic), antiviral (Influenza), antitumor (antineoplastic) 9 > Pa > 0.5 and with a low probability of cytotoxic/cytostatic (cytostatic/cytotoxic) activities. An experimental study by in vitro and in vivo methods allowed us to conclude that studied new synthetic compound N-(β-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effects.

关键词： Biological Activity Synthesis Urea Carbohydrate Compounds Hyperurcemia Ototoxicity Testing Toxicity Anti Tuberculosis Antitumor

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Synthesis, Assessment of Biological Activity and Toxicity for N-(<i>β</i>-D-Glycopyranosyl)-Thiosemicarbazides

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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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