Rare earth chelates of benzoyl urea derivatives were prepared in ethanol and fluorescence spectra of these chelates were studied in detail. A composition of [RE(BU)_3Phen] (NO_3)_3 was obtained. Correlation between ch...Rare earth chelates of benzoyl urea derivatives were prepared in ethanol and fluorescence spectra of these chelates were studied in detail. A composition of [RE(BU)_3Phen] (NO_3)_3 was obtained. Correlation between chemical properties of ligands, chelates and spectroscopy was discussed. Intramolecular energy transfer in rare earth chelates was explained.展开更多
A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened ...A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control. Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib. In particular, 2,6-dimethyl-4-{6-[3-（4-chloro-3-（trifluoromethyl）phenyl）urealnaphthalen- 2-yllsulfonyl morpholine （10d） was found to be the most potent against A375, HepG2 and Ketr3 with ICs0 values of 0.65-0.97 μmol/L, which were 5-20-fold more potent than sorafenib. Compound 10d emerged as a valuable lead for further optimization.展开更多
N-(nitrosomethyl ) urea (NMU ) was characterized in the carcinogenic nitrosated fish sauce (NFS) with high performance liquid chromatography (HPLC )- pholohydrolysis-pyrolysis-thermal en -ergy analysis recently. We us...N-(nitrosomethyl ) urea (NMU ) was characterized in the carcinogenic nitrosated fish sauce (NFS) with high performance liquid chromatography (HPLC )- pholohydrolysis-pyrolysis-thermal en -ergy analysis recently. We used HPLC-electronic spray ionization-mass spectrometry and HPLC-diode array detection to confirm NMU in NFS furiher. It was observed that the corresponding chro-matographic fraction of NMU of NFS showed the same mass spectrum (m/z 64, 102, and 145) andultraviolet-absorbance (λ max = 230 nm) as those of authentic NMU. These results confirmed that thecomponent of NFS was NMU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
Two novel photochromic macrocycles 1 and 2 bearing dithienylethene units and urea building blocks have been synthesized, and their photochromic properties are described. Macrocycle 2 shows good photochromic properties...Two novel photochromic macrocycles 1 and 2 bearing dithienylethene units and urea building blocks have been synthesized, and their photochromic properties are described. Macrocycle 2 shows good photochromic properties, while the relatively smaller size of macrocycle 8h exhibits photochemically inactive properties due to the unfa- vourable ring conformational constraint. Moreover, the crystal structures of the urea-protected precursor macrocyles 3a, 3h, and 8b are presented.展开更多
文摘Rare earth chelates of benzoyl urea derivatives were prepared in ethanol and fluorescence spectra of these chelates were studied in detail. A composition of [RE(BU)_3Phen] (NO_3)_3 was obtained. Correlation between chemical properties of ligands, chelates and spectroscopy was discussed. Intramolecular energy transfer in rare earth chelates was explained.
基金financially supported by the National Science&Technology Major Project(2009ZX09301-003-9-1)
文摘A novel series of diaryl urea derivatives bearing sulfonamide moiety have been designed and synthesized. Their in vitro antitumor effect against human cancer cell lines MX-1, A375, HepG2, Ketr3 and HT-29 was screened and evaluated by the standard MTT assay with sorafenib as the positive control. Some of the compounds showed significant inhibitory activity against multiple cell lines compared to sorafenib. In particular, 2,6-dimethyl-4-{6-[3-（4-chloro-3-（trifluoromethyl）phenyl）urealnaphthalen- 2-yllsulfonyl morpholine （10d） was found to be the most potent against A375, HepG2 and Ketr3 with ICs0 values of 0.65-0.97 μmol/L, which were 5-20-fold more potent than sorafenib. Compound 10d emerged as a valuable lead for further optimization.
文摘N-(nitrosomethyl ) urea (NMU ) was characterized in the carcinogenic nitrosated fish sauce (NFS) with high performance liquid chromatography (HPLC )- pholohydrolysis-pyrolysis-thermal en -ergy analysis recently. We used HPLC-electronic spray ionization-mass spectrometry and HPLC-diode array detection to confirm NMU in NFS furiher. It was observed that the corresponding chro-matographic fraction of NMU of NFS showed the same mass spectrum (m/z 64, 102, and 145) andultraviolet-absorbance (λ max = 230 nm) as those of authentic NMU. These results confirmed that thecomponent of NFS was NMU
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.
基金the National Natural Science Foundation of China，the Natural Science Foundation of Jiangsu Province
文摘Two novel photochromic macrocycles 1 and 2 bearing dithienylethene units and urea building blocks have been synthesized, and their photochromic properties are described. Macrocycle 2 shows good photochromic properties, while the relatively smaller size of macrocycle 8h exhibits photochemically inactive properties due to the unfa- vourable ring conformational constraint. Moreover, the crystal structures of the urea-protected precursor macrocyles 3a, 3h, and 8b are presented.
