The title compound C18H22N4O4 was synthesized by the reaction of 3-hydrazine-4-hydroxy-6-methyl-2（1H）-pyridinones with 2-hydroxy-4-diethylaminobenzaldehyde in ethanol and characteri- zed by IR, tH NMR and elemental ...The title compound C18H22N4O4 was synthesized by the reaction of 3-hydrazine-4-hydroxy-6-methyl-2（1H）-pyridinones with 2-hydroxy-4-diethylaminobenzaldehyde in ethanol and characteri- zed by IR, tH NMR and elemental analysis. The single-crystal structure has been determined by X-ray diffraction analysis. The crystal belongs to the triclinic system, space group P1^- with a = 10.1930（14）, b = 12.5200（17）, c = 15.1863（19） A, α= 96.292（3）, β= 96.450（3）, γ= 102.443（3）°, V= 1862.6（4） A^3, Z= 4, Mr = 358.40, μ = 0.092 mm^-1, D c= 1.278 g/cm^3, F（000） = 760 and R = 0.0803. The crystal structure involves intermolcular N-H…O as well as intramolcular O-H…N, O-H…O and N-H…O hydrogen bonds. The title compound shows no antibacterial activity.展开更多
The title complex [Cu3L3(H2O)]DMFH2O (H2L = 4-(3-hydroxy-2-ethyl-4- pyridinone-1-yl)-aniline condensation salicylaldehyde) was obtained. The single-crystal X-ray study shows that it is a trinuclear compound [Cu3(C20H1...The title complex [Cu3L3(H2O)]DMFH2O (H2L = 4-(3-hydroxy-2-ethyl-4- pyridinone-1-yl)-aniline condensation salicylaldehyde) was obtained. The single-crystal X-ray study shows that it is a trinuclear compound [Cu3(C20H15N2O3)3(H2O)]DMFH2O. The coordi- nation sphere about each copper ion in the complex consists of two oxygen atoms from hydroxylpyridinone moiety of one ligand and one oxygen and one nitrogen atoms from salicyladehyde Schiff-base moiety of another ligand arranged in a slightly distorted square planar geometry. Among the three copper ions, one (Cu(2)) is coordinated by the other oxygen atom of water molecule on the fifth coordinate position to form a distorted square pyramid geometry. The crystal is of monoclinic, space group P21/c with a = 12.9202(5), b = 27.197(1), c = 17.0116(7) ? b = 100.588(1), V = 5875.9(4) 3, Z = 4, C63H57N7O12Cu3, Mr = 1294.78, Dc = 1.464 g/cm3, m = 1.146 mm-1, F(000) = 2668, R = 0.0784 and wR = 0.1546 for 6926 observed reflections with I > 2s(I). The differences of coordinate bond lengths are observed between anhydrous and hydrous units: in the former unit, the average bond lengths are 1.978 ?for CuN (azomethine), 1.883 ?for CuO (phenolic) in Schiff-base moiety, 1.959 ?for CuO (keto), and 1.919 ?for CuO (hydroxy) in hydroxypyridinone moiety; while those in the latter are longer with the following corresponding values: 1.985(5), 1.908(5), 1.993(5) and 1.919(4) ? respectively. The Cu(2)O (water) bond length is 2.375(6) ?展开更多
The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzyliden...The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944（19）, b = 10.5250（3）, c = 24.4985（6） A, Z = 4, V = 2041.66（9） A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F（000） = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O（2）-H（2A）…O（1）, O（2）-H（2B）…N（I） and N（5）-H（5）…O（2）, and an octatomic ring R^（8） is formed via intramolecular hydrogen bond of O（I）-H（IA）…N（4）. Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.展开更多
(R)-1,3-butanediol is an important pharmaceutical intermediate, and the synthesis of(R)-1,3-butanediol using green biological methods has recently been of interest for industrial application. Here, a novel strain QC-1...(R)-1,3-butanediol is an important pharmaceutical intermediate, and the synthesis of(R)-1,3-butanediol using green biological methods has recently been of interest for industrial application. Here, a novel strain QC-1 that efficiently transforms 4-hydroxy-2-butanone to(R)-1,3-butanediol was isolated from soil samples. Based on morphological, physiological, and biochemical tests and 5.8 S-internal transcribed spacer sequencing, the strain was identified as Pichia kudriavzevii QC-1. The reaction conditions were optimized to 35 ℃, pH 8.0, rotation speed 200 rpm, and 6:5 mass ratio of glucose to 4-hydroxy-2-butanone. Evaluation of the effects of 4-hydroxy-2-butanone concentrations on yield and cell survival rate showed that 85.60 g·L^-1 product accumulated, with an enantiomeric excess of more than 99%, when 30 g·L^-14-hydroxy-2-butanone was added at 0, 10, and 30 h in a 3-L bioreactor. Thus, strain QC-1 showed excellent catalytic activity and stereoselectivity for the synthesis of(R)-1,3-butanediol from 4-hydroxy-2-butanone.展开更多
Liver diseases with the central pathogenetic mechanism of oxidative stress are one of the main causes of mortality worldwide.Therefore,dihydroquinoline derivatives,which are precursors of hepatoprotectors and have ant...Liver diseases with the central pathogenetic mechanism of oxidative stress are one of the main causes of mortality worldwide.Therefore,dihydroquinoline derivatives,which are precursors of hepatoprotectors and have antioxidant activity,are of interest.We have previously found that some compounds in this class have the ability to normalize redox homeostasis under experimental conditions.Here,we initially analyzed the hepatoprotective potential of the dihydroquinoline derivative 1-benzoyl-6-hydroxy-2,2,4-trimethyl-1,2-dihydroquinoline(BHDQ)for carbon tetrachloride(CCl4)-induced liver injury in rats.Results suggested that BHDQ normalized the alanine aminotransferase,aspartate aminotransferase,and gamma-glutamyl transpeptidase in serum.We also observed an improvement in liver tissue morphology related to BHDQ.Animals with CCl4-induced liver injuries treated with BHDQ had less oxidative stress compared to animals with CCl4-induced liver injury.BHDQ promoted activation changes in superoxide dismutase,catalase,glutathione peroxidase,glutathione reductase,and glutathione transferase on control values in animals with CCl4-induced liver injury.BHDQ also activated gene transcription in Sod1 and Gpx1 via nuclear factor erythroid 2-related factor 2 and forkhead box protein O1 factors.Therefore,the compound of concern has a hepatoprotective effect by inhibiting the development of necrotic processes in the liver tissue,through antioxidation.展开更多
3,4-Dihydropyrimidin-2-(1H)-ones were synthesized in high yields by a one-pot cyclocondensation of aldehyde,1,3-dicarbonyl compound,and urea or thiourea using copper o-toluenesulfonate as a catalyst under solvent-free...3,4-Dihydropyrimidin-2-(1H)-ones were synthesized in high yields by a one-pot cyclocondensation of aldehyde,1,3-dicarbonyl compound,and urea or thiourea using copper o-toluenesulfonate as a catalyst under solvent-free conditions at 90℃.Effects of molar ratio of reactants,amount of catalyst,and reaction temperature on the yields of 3,4-dihydropyrimidin-2-(1H)-ones were investigated.The results showed that at the condition of naldehyde∶n1,3-dicarbonyl compounds∶nurea(or thiourea)=1∶1.2∶1.5,1 mol% catalyst(molar percent of aldehyde),2.0 h at 90℃,the yields of products were 51-96%.After reaction,the catalyst could be reused for four times without distinct loss of catalytic activity.展开更多
Dihydroquinazolin-4(3H)-ones were synthesized by the reaction of o-nitrobenzamides with aromatic aldehydes or cyclones promoted by the low-valent titanium reagent(TiCl 4-Zn system). The products were characterized by ...Dihydroquinazolin-4(3H)-ones were synthesized by the reaction of o-nitrobenzamides with aromatic aldehydes or cyclones promoted by the low-valent titanium reagent(TiCl 4-Zn system). The products were characterized by elementary analysis, IR, 1H NMR and X-ray single crystal diffraction. This method possesses the advantages of easily accessible starting materials, convenient manipulation and moderate to high yields.展开更多
基金This work was supported by the Natural Science Foundation of Zhejiang Province (No. M203115) and Scientific Research Fund of Zhejiang Provincial Education Department (No. 20050057, 20050051)
文摘The title compound C18H22N4O4 was synthesized by the reaction of 3-hydrazine-4-hydroxy-6-methyl-2（1H）-pyridinones with 2-hydroxy-4-diethylaminobenzaldehyde in ethanol and characteri- zed by IR, tH NMR and elemental analysis. The single-crystal structure has been determined by X-ray diffraction analysis. The crystal belongs to the triclinic system, space group P1^- with a = 10.1930（14）, b = 12.5200（17）, c = 15.1863（19） A, α= 96.292（3）, β= 96.450（3）, γ= 102.443（3）°, V= 1862.6（4） A^3, Z= 4, Mr = 358.40, μ = 0.092 mm^-1, D c= 1.278 g/cm^3, F（000） = 760 and R = 0.0803. The crystal structure involves intermolcular N-H…O as well as intramolcular O-H…N, O-H…O and N-H…O hydrogen bonds. The title compound shows no antibacterial activity.
基金This work was supported by the foundation of Natural Science Research of Jiangsu Education Department (02KJB150007)
文摘The title complex [Cu3L3(H2O)]DMFH2O (H2L = 4-(3-hydroxy-2-ethyl-4- pyridinone-1-yl)-aniline condensation salicylaldehyde) was obtained. The single-crystal X-ray study shows that it is a trinuclear compound [Cu3(C20H15N2O3)3(H2O)]DMFH2O. The coordi- nation sphere about each copper ion in the complex consists of two oxygen atoms from hydroxylpyridinone moiety of one ligand and one oxygen and one nitrogen atoms from salicyladehyde Schiff-base moiety of another ligand arranged in a slightly distorted square planar geometry. Among the three copper ions, one (Cu(2)) is coordinated by the other oxygen atom of water molecule on the fifth coordinate position to form a distorted square pyramid geometry. The crystal is of monoclinic, space group P21/c with a = 12.9202(5), b = 27.197(1), c = 17.0116(7) ? b = 100.588(1), V = 5875.9(4) 3, Z = 4, C63H57N7O12Cu3, Mr = 1294.78, Dc = 1.464 g/cm3, m = 1.146 mm-1, F(000) = 2668, R = 0.0784 and wR = 0.1546 for 6926 observed reflections with I > 2s(I). The differences of coordinate bond lengths are observed between anhydrous and hydrous units: in the former unit, the average bond lengths are 1.978 ?for CuN (azomethine), 1.883 ?for CuO (phenolic) in Schiff-base moiety, 1.959 ?for CuO (keto), and 1.919 ?for CuO (hydroxy) in hydroxypyridinone moiety; while those in the latter are longer with the following corresponding values: 1.985(5), 1.908(5), 1.993(5) and 1.919(4) ? respectively. The Cu(2)O (water) bond length is 2.375(6) ?
基金supported by the National Undergraduate Training Programs for Innovation and Entrepreneurship of Hunan Universitythe Natural Science Foundation of Hunan Province(No.12jj3012)
文摘The title compound, 4-（tert-butyl）-5-（1 H- 1,2,4-triazol- 1 -yl）-N-（2-hydroxy-3,5-diio- dinebenzyl）thiazol-2-amine, was synthesized via the reduction of 4-（tert-butyl）-5-（1H-l,2,4- triazol-l-yl）-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944（19）, b = 10.5250（3）, c = 24.4985（6） A, Z = 4, V = 2041.66（9） A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F（000） = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections （I 〉 2σ（I））. X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O（2）-H（2A）…O（1）, O（2）-H（2B）…N（I） and N（5）-H（5）…O（2）, and an octatomic ring R^（8） is formed via intramolecular hydrogen bond of O（I）-H（IA）…N（4）. Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.
基金Financial supports from the National Key R&D Program of China(2018YFC1604100)the National Natural Science Foundation of China(NSFC)[21676120,31872891]+8 种基金the 111 Project[111-2-06]the Highend Foreign Experts Recruitment Program[G20190010083]the Program for Advanced Talents within Six Industries of Jiangsu Province[2015-NY007]the National Program for Support of Top-notch Young Professionalsthe Fundamental Research Funds for the Central Universities[JUSRP51504]the Project Funded by the Priority Academic Program Development of Jiangsu Higher Education InstitutionsTop-notch Academic Programs Project of Jiangsu Higher Education Institutionsthe Jiangsu Province“Collaborative Innovation Center for Advanced Industrial Fermentation”Industry Development Programthe National First-Class Discipline Program of Light Industry Technology and Engineering[LITE2018-09]。
文摘(R)-1,3-butanediol is an important pharmaceutical intermediate, and the synthesis of(R)-1,3-butanediol using green biological methods has recently been of interest for industrial application. Here, a novel strain QC-1 that efficiently transforms 4-hydroxy-2-butanone to(R)-1,3-butanediol was isolated from soil samples. Based on morphological, physiological, and biochemical tests and 5.8 S-internal transcribed spacer sequencing, the strain was identified as Pichia kudriavzevii QC-1. The reaction conditions were optimized to 35 ℃, pH 8.0, rotation speed 200 rpm, and 6:5 mass ratio of glucose to 4-hydroxy-2-butanone. Evaluation of the effects of 4-hydroxy-2-butanone concentrations on yield and cell survival rate showed that 85.60 g·L^-1 product accumulated, with an enantiomeric excess of more than 99%, when 30 g·L^-14-hydroxy-2-butanone was added at 0, 10, and 30 h in a 3-L bioreactor. Thus, strain QC-1 showed excellent catalytic activity and stereoselectivity for the synthesis of(R)-1,3-butanediol from 4-hydroxy-2-butanone.
基金supported by the Russian Foundation for Basic Research (Grant No. 20-04-00526А)
文摘Liver diseases with the central pathogenetic mechanism of oxidative stress are one of the main causes of mortality worldwide.Therefore,dihydroquinoline derivatives,which are precursors of hepatoprotectors and have antioxidant activity,are of interest.We have previously found that some compounds in this class have the ability to normalize redox homeostasis under experimental conditions.Here,we initially analyzed the hepatoprotective potential of the dihydroquinoline derivative 1-benzoyl-6-hydroxy-2,2,4-trimethyl-1,2-dihydroquinoline(BHDQ)for carbon tetrachloride(CCl4)-induced liver injury in rats.Results suggested that BHDQ normalized the alanine aminotransferase,aspartate aminotransferase,and gamma-glutamyl transpeptidase in serum.We also observed an improvement in liver tissue morphology related to BHDQ.Animals with CCl4-induced liver injuries treated with BHDQ had less oxidative stress compared to animals with CCl4-induced liver injury.BHDQ promoted activation changes in superoxide dismutase,catalase,glutathione peroxidase,glutathione reductase,and glutathione transferase on control values in animals with CCl4-induced liver injury.BHDQ also activated gene transcription in Sod1 and Gpx1 via nuclear factor erythroid 2-related factor 2 and forkhead box protein O1 factors.Therefore,the compound of concern has a hepatoprotective effect by inhibiting the development of necrotic processes in the liver tissue,through antioxidation.
文摘3,4-Dihydropyrimidin-2-(1H)-ones were synthesized in high yields by a one-pot cyclocondensation of aldehyde,1,3-dicarbonyl compound,and urea or thiourea using copper o-toluenesulfonate as a catalyst under solvent-free conditions at 90℃.Effects of molar ratio of reactants,amount of catalyst,and reaction temperature on the yields of 3,4-dihydropyrimidin-2-(1H)-ones were investigated.The results showed that at the condition of naldehyde∶n1,3-dicarbonyl compounds∶nurea(or thiourea)=1∶1.2∶1.5,1 mol% catalyst(molar percent of aldehyde),2.0 h at 90℃,the yields of products were 51-96%.After reaction,the catalyst could be reused for four times without distinct loss of catalytic activity.
文摘Dihydroquinazolin-4(3H)-ones were synthesized by the reaction of o-nitrobenzamides with aromatic aldehydes or cyclones promoted by the low-valent titanium reagent(TiCl 4-Zn system). The products were characterized by elementary analysis, IR, 1H NMR and X-ray single crystal diffraction. This method possesses the advantages of easily accessible starting materials, convenient manipulation and moderate to high yields.
基金Postdoctoral Science Foundation of China(2012M520605)Research Foundation of Taiyuan University of Technology(tyut-rc201369a,2013Z040)+1 种基金Open Foundation of State Key Laboratory of Coal Conversion(09-102)Natural Science Foundation of Shanxi Province(2013011042-1)
