A series of new 1-aryloxyacetyl-4-aroylthiosemicarbazides were synthesized by means of solid-liguid phase transfer catalysis. The promoting effects of these new compounds on wheat growth were observed.
Synthesis and antibacterial activity of some novel urea and thiourea derivatives (8a - 8k, 9a - 9f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew N...Synthesis and antibacterial activity of some novel urea and thiourea derivatives (8a - 8k, 9a - 9f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut Shell Liquid (CNSL). Compounds (8a - 8k, 9a - 9f) were tested for Gram positive and Gram negative bacterial cultures. Most of the compounds were showed active compared with standard drug ampicilline.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
Synthesis and antibacterial activity of some novel urea and thiourea derivatives (7a-7k, 8a-8f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut S...Synthesis and antibacterial activity of some novel urea and thiourea derivatives (7a-7k, 8a-8f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut Shell Liquid (CNSL). Compounds (7a-7k, 8a-8f) were tested for Gram positive and Gram negative bac- terial cultures. Most of the compounds were showed active compared with standard drug ampicilline.展开更多
A series of novel phenothiazine derivatives was synthesized and tested for arginine vasopressin receptor antagonist activity. They were synthesized as novel arginine vasopressin receptor antagonists from phenothiazine...A series of novel phenothiazine derivatives was synthesized and tested for arginine vasopressin receptor antagonist activity. They were synthesized as novel arginine vasopressin receptor antagonists from phenothiazine as a scaffold via successive acylation, reduction and acylation reactions. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS, and biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay indicated that several compounds are potent selective V2 receptor antagonists. Compounds with promising binding affinity to V2 receptors were selected to conduct the in vivo diuretic studies on Sprague-Dawley rats. Among them, 1n, 1r, It and 1v exhibited excellent diuretic activity, especially 1 r and 1v. Therefore, 1 r and 1v are potent novel AVP V2 receptor antagonist candidates.展开更多
In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moietie...In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moieties of the cordycepin analogs that were required for antitumor activity.Among all the target compounds,those with 4-methyl and 4-nitro substituents on the benzene ring displayed better activity than the lead compound in antiproliferative activity experiments using MDA-MB-231 and A549 cells.However,compounds with 4-methoxybenzene and 2-oxoindoline groups and ethylene spacers displayed more significant activity than the lead compound in antiproliferative activity experiments using He La cells.In particular,a compound with a 4-bromo substituent and an ethylene spacer displayed very high inhibitory activity against the proliferation of MDA-MB-231,A549,and He La cells,suggesting that it had the potential for further development and application.展开更多
基金This project was supported by Nature Science Foundation of Gansu.
文摘A series of new 1-aryloxyacetyl-4-aroylthiosemicarbazides were synthesized by means of solid-liguid phase transfer catalysis. The promoting effects of these new compounds on wheat growth were observed.
文摘Synthesis and antibacterial activity of some novel urea and thiourea derivatives (8a - 8k, 9a - 9f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut Shell Liquid (CNSL). Compounds (8a - 8k, 9a - 9f) were tested for Gram positive and Gram negative bacterial cultures. Most of the compounds were showed active compared with standard drug ampicilline.
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Synthesis and antibacterial activity of some novel urea and thiourea derivatives (7a-7k, 8a-8f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut Shell Liquid (CNSL). Compounds (7a-7k, 8a-8f) were tested for Gram positive and Gram negative bac- terial cultures. Most of the compounds were showed active compared with standard drug ampicilline.
基金supported by National Major Scientific and Technological Special Project for "Significant New Drugs Development"(Nos.2011ZX09401-009 and 2013ZX09102014)
文摘A series of novel phenothiazine derivatives was synthesized and tested for arginine vasopressin receptor antagonist activity. They were synthesized as novel arginine vasopressin receptor antagonists from phenothiazine as a scaffold via successive acylation, reduction and acylation reactions. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS, and biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay indicated that several compounds are potent selective V2 receptor antagonists. Compounds with promising binding affinity to V2 receptors were selected to conduct the in vivo diuretic studies on Sprague-Dawley rats. Among them, 1n, 1r, It and 1v exhibited excellent diuretic activity, especially 1 r and 1v. Therefore, 1 r and 1v are potent novel AVP V2 receptor antagonist candidates.
基金Research Basic Ability Enhancement Project of Young and Middle-aged Teachers in Guangxi Universities(Grant No.2019KY0166)the Project of Guangxi University for Nationalities(Grant No.2018MDYB006,2018XJGY46)。
文摘In this study,a novel series of cordycepin derivatives with benzenesulfonamido groups at the 6-position of the purine ring were synthesized and their antitumor activity was evaluated.We revealed the structural moieties of the cordycepin analogs that were required for antitumor activity.Among all the target compounds,those with 4-methyl and 4-nitro substituents on the benzene ring displayed better activity than the lead compound in antiproliferative activity experiments using MDA-MB-231 and A549 cells.However,compounds with 4-methoxybenzene and 2-oxoindoline groups and ethylene spacers displayed more significant activity than the lead compound in antiproliferative activity experiments using He La cells.In particular,a compound with a 4-bromo substituent and an ethylene spacer displayed very high inhibitory activity against the proliferation of MDA-MB-231,A549,and He La cells,suggesting that it had the potential for further development and application.
