This work is describing a thionization method for glycosyl urea and carbamide of sugars by using the Lawesson’s reagent. It is proposed the method based on the interaction of glycosyl urea and carbamide of sugars wit...This work is describing a thionization method for glycosyl urea and carbamide of sugars by using the Lawesson’s reagent. It is proposed the method based on the interaction of glycosyl urea and carbamide of sugars with the Lawessons reagent at a 1:1 ratio in the presence of a pyridine. As a result, sulfur-containing derivatives of sugar carbamides are obtained with the help of Lawesson’s reagent. Obtained experimental data are indicating the developed new method for thionization of sugar carbamides, which opens up broad possibilities for synthesis of various carbohydrate derivatives of thiourea. Significance of this work is that, thiourea derivatives are promising bactericidal, fungicidal and anti-inflammatory drugs. Therefore, the preparation of thiourea derivatives and the study of their properties remain topical tasks in the field of chemistry.展开更多
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-(<em>β</em>-D...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-(<em>β</em>-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-(<em>β</em>-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-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazides, the probability of pharmacological and toxic effects were predicted by the computer method in silico. From the synthesized compounds N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide, the probability of antibacterial (antibacterial) activity is predicted (<em>Pa</em>/<em>Pi</em> 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-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effect. The synthetic new compound N-(<em>β</em>-D-glyco- pyranosyl)-thiosemicarbazide is a promising compound for further study.展开更多
Computer analysis of N-(β-D-galactopyranosyl)-thiosemicarbazide compounds by in silico method revealed high probability of antibacterial (antimycobacterial), anti-tuberculosis (antituberculosic), antiviral (Influenza...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.展开更多
文摘This work is describing a thionization method for glycosyl urea and carbamide of sugars by using the Lawesson’s reagent. It is proposed the method based on the interaction of glycosyl urea and carbamide of sugars with the Lawessons reagent at a 1:1 ratio in the presence of a pyridine. As a result, sulfur-containing derivatives of sugar carbamides are obtained with the help of Lawesson’s reagent. Obtained experimental data are indicating the developed new method for thionization of sugar carbamides, which opens up broad possibilities for synthesis of various carbohydrate derivatives of thiourea. Significance of this work is that, thiourea derivatives are promising bactericidal, fungicidal and anti-inflammatory drugs. Therefore, the preparation of thiourea derivatives and the study of their properties remain topical tasks in the field of chemistry.
文摘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-(<em>β</em>-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-(<em>β</em>-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-(<em>β</em>-D-glycopyranosyl)-thiosemicarbazides, the probability of pharmacological and toxic effects were predicted by the computer method in silico. From the synthesized compounds N-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide, the probability of antibacterial (antibacterial) activity is predicted (<em>Pa</em>/<em>Pi</em> 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-(<em>β</em>-D-galactopyranosyl)-thiosemicarbazide in the studied concentrations has a pronounced bactericidal and bacteriostatic effect. The synthetic new compound N-(<em>β</em>-D-glyco- pyranosyl)-thiosemicarbazide is a promising compound for further study.
文摘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.
