A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus （HBV） activities were ...A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus （HBV） activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ （ 3-methoxyphenylsulfinyl ） methyl ] -1-methyl-4- [ （4-methylpiperazin-1-yl） methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.展开更多
2,2'-Arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) 4l-s produced from reaction between dimedone with various aldehydes in acetonitrile using ZnO as a catalyst;whereas in the presence of ZnO-acetyl ...2,2'-Arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) 4l-s produced from reaction between dimedone with various aldehydes in acetonitrile using ZnO as a catalyst;whereas in the presence of ZnO-acetyl chloride catalysts the reaction is limited to give only 1,8-dioxo-octahydroxanthenes 3a-k in very good yields.展开更多
The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized...The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.展开更多
A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid recep...A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. Hematoxylin-eosin staining and a terminal deoxynucleotidyl transferase dUTP nick end labeling assay showed that retinal ganglion cells gradually decreased with increasing time of optic nerve injury, while GYKI 52466 could inhibit this process. The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist.展开更多
2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group ...2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group in 1 binding to CPA,2-benzyl-5- benzyloxy-4-oxopentanoic acid 2 was also synthesized and evaluated.The inhibition constants show that both L-1 and D-1 were shown to have strong binding affinity with L-1 being more potent than its enantiomer by 165-fold.On the other hand,the inhibition constant ...展开更多
One novel nickel coordination polymer, {[Ni（OTP）（bib）1.5（H2O）]·2H2O}n（1, H2 OTP = 2-hydroxy-5-（3＇,5＇-terephthalic acid） pyridine, bib = 1,4-bis（1-imdazoly）benzene）, has been synthesized and characte...One novel nickel coordination polymer, {[Ni（OTP）（bib）1.5（H2O）]·2H2O}n（1, H2 OTP = 2-hydroxy-5-（3＇,5＇-terephthalic acid） pyridine, bib = 1,4-bis（1-imdazoly）benzene）, has been synthesized and characterized by elemental analysis（EA）, IR, powder X-ray diffraction（PXRD）, and thermogravimetric（TG） analyses. The crystal of 1 crystallizes in monoclinic, space group P21/n with a = 12.2860（5）, b = 13.8246（6）, c = 19.0140（8） A, β = 104.3870（1）°, V = 3128.2（2） A3, Z = 4, C32H28N7 Ni O8, Mr = 697.32, Dc = 1.481 g/cm^3, F（000） = 1444 and μ（Mo Kα） = 0.684 mm-1. The final R = 0.0704 and w R = 0.1764 for 5485 observed reflections with I 2σ（I） and R = 0.1087 and wR = 0.2010 for all data. Topology analysis reveals that complex 1 is a 3D 2-fold interpenetrated {4^4·6^6}-nov net based on the 1D [Ni（OTP）]n chain and the 2D [Ni2（bib）3]n sql sheet. And the variable-temperature magnetic susceptibility measurements exhibit weak antiferromagnetic coupling interaction.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
A facile and efficient synthesis of (+)-5α-hydroxy -β-selinene 1 and (-)-5β-hydroxy-β-selinene 2 starting from (+)-dihydrocarvone 3 has been described.
（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-...（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-5-hydroxy-2（E）-hexenoate in good yield with over 99% e.e..展开更多
5-Hydroxy-2-（2-phenylethyl）chromone（l） was synthesized from 2,6-dihydroxyacetophenone（7） obtained via four-steps resorcinol-reacting with phenylpropionic acid, the procedures involved are Baker-Venkataraman rear...5-Hydroxy-2-（2-phenylethyl）chromone（l） was synthesized from 2,6-dihydroxyacetophenone（7） obtained via four-steps resorcinol-reacting with phenylpropionic acid, the procedures involved are Baker-Venkataraman rear-rangement and cyclization which are easy to conduct, the overall yield is 32%.展开更多
A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric ...A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric pressure. The test indicated a relatively high activity of the HZSM-5 zeolite capable of achieving a HH conversion of 99.2% and a HO yield of 83.5%. Catalyst deactivation could be prevented by increasing the reaction temperature by 10 ＂C for every 20 h and adding 2.0% of piperidine in the feed. A catalyst stability test （for 100 h） in FBR showed that the catalyst was active even after 100 h of time-on-stream with HH conversion remaining at 99.2% and HO yield still reaching over 83.5%. Regenera- tion experiment showed that the regenerated catalyst demonstrated a catalytic performance comparable to the fresh one.展开更多
The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crysta...The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the monoclinic system, space group C2/c with a = 4.4026（6）, b = 1.501（13）, c = 0.95818（12） nm, β = 90.868（2）°, V= 4.2813（9） nm^3, Z= 8, Dc= 1.292 g/cm^3,μ = 0.010, F（000） = 1744, R = 0.0576 and wR = 0.1450 for 3766 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the molecule has a pair of intramolecular OH…N hydrogen bonds.展开更多
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） acti...A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine（IC50=54.78μmol/L）.展开更多
A kinetie method is described for the determination of trace amounts of mangancsc (Ⅱ)based on its catalylic effect on the aerial oxidation of 1.5-bis (2-hydroxy-5-chlorophenyl)-3-cyanofrmazan. The reaction is followe...A kinetie method is described for the determination of trace amounts of mangancsc (Ⅱ)based on its catalylic effect on the aerial oxidation of 1.5-bis (2-hydroxy-5-chlorophenyl)-3-cyanofrmazan. The reaction is followed spectrophotometrically by measurin the rate of change in absorbance at 580nm. The calibration curve (rate constant vs. manganese concentration) is linearin the range of 10~200ng in 25ml solutions. Kinetic parameters of the reaction are reported. Thereare few Interferences.展开更多
A facile synthesis of the analog of curcumin. 1,7-bis (4-hydroxyphenyl)-3-hydroxy-1.3-heptadien-5-one 1 was achieved. The key step was completed through the regioselective condensation of ketone 5 and acyl chloride 7.
A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structur...A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structurally characterized by single-crystal X-ray diffrac- tion, infrared （IR） spectra, elemental analysis, powder X-ray diffractions （PXRD） and thermo- gravimetric analysis （TGA）. Compound 1 crystallizes in monoclinic, space group P2Jc with a = 14.6525（9）, b = 13.3917（9）, c = 11.8838（8） A, β = 101.2290（10）°, V = 2287.2（3） A3, Z = 4, C20H24CdN6OsS, Mr = 572.91, Dc. = 1.664 mg-mm-3, F（000） = 1160, p = 1.091 mm-1, R = 0.0232 and wR = 0.0587 for 3597 observed reflections （I 〉 2σ（I））. Compound 1 exhibits a one-dimensional （1D） double-chain structure which is further connected through hydrogen bonding and π-π interactions into a three-dimensional （3D） supramolecular network. In addition, it exhibits blue fluorescence at room temperature in the solid state.展开更多
Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic pos...Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic postsurgical pain. However, it is unclear how chronification of postsurgical pain occurs. The α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor(AMPA) phosphorylation in the central nervous system plays a critical role in synaptic plasticity and contributes to central sensitization and chronic pain development. Here, we discuss the role of AMPA receptor regulation in stress-induced pain chronification after surgery.展开更多
The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental ana...The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673（8）, b = 17.9938（15）, c = 21.2004（17） A, V = 3611.5（5） A3, Z = 8, μ = 0.6726 mm^（-1）, Dc = 1.795 g/cm3, F（000） = 2080, the final R = 0.0358 and wR = 0.0644 with I 2σ（I）. The results show that the addition reaction occurs at the carbon-carbon double bond（C2 and C3） of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells（K562）, human breast cancer cells（MCF-7） and human lung cancer cells（A549）. 1 exhibited potent antitumor activities against human leukemia cells（K562） with the IC50 values of 18.9 μmol/L.展开更多
基金Supported by the National Natural Science Foundation of China(No.20042047).
文摘A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus （HBV） activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ （ 3-methoxyphenylsulfinyl ） methyl ] -1-methyl-4- [ （4-methylpiperazin-1-yl） methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.
基金support from the Research Council of University of Sistan and Baluchestan, Iran
文摘2,2'-Arylmethylene bis(3-hydroxy-5,5-dimethyl-2-cyclohexene-1-one) 4l-s produced from reaction between dimedone with various aldehydes in acetonitrile using ZnO as a catalyst;whereas in the presence of ZnO-acetyl chloride catalysts the reaction is limited to give only 1,8-dioxo-octahydroxanthenes 3a-k in very good yields.
文摘The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.
基金The Foundation of Xinjiang Uygur Autonomous Region in China, No. 200821137the National Natural Science Foundation of China, No. 81160153
文摘A rabbit model of traumatic optic nerve injury, established by occlusion of the optic nerve using a vascular clamp, was used to investigate the effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist GYKI 52466 on apoptosis of retinal ganglion cells following nerve injury. Hematoxylin-eosin staining and a terminal deoxynucleotidyl transferase dUTP nick end labeling assay showed that retinal ganglion cells gradually decreased with increasing time of optic nerve injury, while GYKI 52466 could inhibit this process. The results demonstrate that following acute optic nerve injury, apoptosis of retinal ganglion cells is a programmed process, which can be inhibited by the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist.
文摘2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group in 1 binding to CPA,2-benzyl-5- benzyloxy-4-oxopentanoic acid 2 was also synthesized and evaluated.The inhibition constants show that both L-1 and D-1 were shown to have strong binding affinity with L-1 being more potent than its enantiomer by 165-fold.On the other hand,the inhibition constant ...
基金supported by the Natural Science Foundation of Shandong Province(ZR2011BL020,ZR2012CM019)National Natural Science Foundation of China(21451001)Key Discipline and Innovation Team of Qilu Normal University
文摘One novel nickel coordination polymer, {[Ni（OTP）（bib）1.5（H2O）]·2H2O}n（1, H2 OTP = 2-hydroxy-5-（3＇,5＇-terephthalic acid） pyridine, bib = 1,4-bis（1-imdazoly）benzene）, has been synthesized and characterized by elemental analysis（EA）, IR, powder X-ray diffraction（PXRD）, and thermogravimetric（TG） analyses. The crystal of 1 crystallizes in monoclinic, space group P21/n with a = 12.2860（5）, b = 13.8246（6）, c = 19.0140（8） A, β = 104.3870（1）°, V = 3128.2（2） A3, Z = 4, C32H28N7 Ni O8, Mr = 697.32, Dc = 1.481 g/cm^3, F（000） = 1444 and μ（Mo Kα） = 0.684 mm-1. The final R = 0.0704 and w R = 0.1764 for 5485 observed reflections with I 2σ（I） and R = 0.1087 and wR = 0.2010 for all data. Topology analysis reveals that complex 1 is a 3D 2-fold interpenetrated {4^4·6^6}-nov net based on the 1D [Ni（OTP）]n chain and the 2D [Ni2（bib）3]n sql sheet. And the variable-temperature magnetic susceptibility measurements exhibit weak antiferromagnetic coupling interaction.
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.
文摘A facile and efficient synthesis of (+)-5α-hydroxy -β-selinene 1 and (-)-5β-hydroxy-β-selinene 2 starting from (+)-dihydrocarvone 3 has been described.
文摘（＋）-（4S,5R）-and （-）-（4R,5S）-osmundalactones as well as （＋）-（4R,5S）- and （-）-（4S,5R）- 5-hydroxy-2-hexen-4-olides were synthesized by a concise and efficient synthesis method starting from 4-benzyloxy-5-hydroxy-2（E）-hexenoate in good yield with over 99% e.e..
文摘5-Hydroxy-2-（2-phenylethyl）chromone（l） was synthesized from 2,6-dihydroxyacetophenone（7） obtained via four-steps resorcinol-reacting with phenylpropionic acid, the procedures involved are Baker-Venkataraman rear-rangement and cyclization which are easy to conduct, the overall yield is 32%.
基金supported by the Science and Technology Planning Program of Tianjin(Project No.12ZXCXGX21900)
文摘A study on catalytic dehydration of 4-hydroxy-3-hexanone （HH） to 4-hexen-3-one （HO） was carried out through conversion of HH over HZSM-5 zeolite catalyst in a fixed-bed reactor （FBR） operating under almospheric pressure. The test indicated a relatively high activity of the HZSM-5 zeolite capable of achieving a HH conversion of 99.2% and a HO yield of 83.5%. Catalyst deactivation could be prevented by increasing the reaction temperature by 10 ＂C for every 20 h and adding 2.0% of piperidine in the feed. A catalyst stability test （for 100 h） in FBR showed that the catalyst was active even after 100 h of time-on-stream with HH conversion remaining at 99.2% and HO yield still reaching over 83.5%. Regenera- tion experiment showed that the regenerated catalyst demonstrated a catalytic performance comparable to the fresh one.
基金supported by the Project for Distinguished Young Scholars from Hubei Provincial Department of Education (No. Q20082601)
文摘The title compound [2-hydroxy-5-（4-hydroxy-3-phenyliminomethyl-benzyl）-benzylidene]-phenyl-amine （C27H22N2O2, Mr = 406.47） was synthesized by 5,5′-methylene-bissalicylal- dehyde with aminobenezene, and its crystal structure was determined by single-crystal X-ray diffraction. The crystal belongs to the monoclinic system, space group C2/c with a = 4.4026（6）, b = 1.501（13）, c = 0.95818（12） nm, β = 90.868（2）°, V= 4.2813（9） nm^3, Z= 8, Dc= 1.292 g/cm^3,μ = 0.010, F（000） = 1744, R = 0.0576 and wR = 0.1450 for 3766 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the molecule has a pair of intramolecular OH…N hydrogen bonds.
基金Supported by the National Natural Science Foundation of China(No.30672519)
文摘A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus（HBV） activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine（IC50=54.78μmol/L）.
文摘A kinetie method is described for the determination of trace amounts of mangancsc (Ⅱ)based on its catalylic effect on the aerial oxidation of 1.5-bis (2-hydroxy-5-chlorophenyl)-3-cyanofrmazan. The reaction is followed spectrophotometrically by measurin the rate of change in absorbance at 580nm. The calibration curve (rate constant vs. manganese concentration) is linearin the range of 10~200ng in 25ml solutions. Kinetic parameters of the reaction are reported. Thereare few Interferences.
文摘A facile synthesis of the analog of curcumin. 1,7-bis (4-hydroxyphenyl)-3-hydroxy-1.3-heptadien-5-one 1 was achieved. The key step was completed through the regioselective condensation of ketone 5 and acyl chloride 7.
基金National Basic Research Program of China(973 Program,No.2012CB821700)Major International(Regional)Joint Research Project of National Natural Science Foundation(No.21120102034)+2 种基金National Natural Science Foundation(No.2083100251108122)Education Department of Jilin Province(No.2013-328)
文摘A new coordination polymer, {[CdL（en）]＇DMF}n （1, H2L = 4-[（8-hydroxy-5- quinolinyl）azo]-benzenesulfonic acid, en = ethylenediamine, DMF = N,N-dimethylformamide）, has been solvothermally synthesized and structurally characterized by single-crystal X-ray diffrac- tion, infrared （IR） spectra, elemental analysis, powder X-ray diffractions （PXRD） and thermo- gravimetric analysis （TGA）. Compound 1 crystallizes in monoclinic, space group P2Jc with a = 14.6525（9）, b = 13.3917（9）, c = 11.8838（8） A, β = 101.2290（10）°, V = 2287.2（3） A3, Z = 4, C20H24CdN6OsS, Mr = 572.91, Dc. = 1.664 mg-mm-3, F（000） = 1160, p = 1.091 mm-1, R = 0.0232 and wR = 0.0587 for 3597 observed reflections （I 〉 2σ（I））. Compound 1 exhibits a one-dimensional （1D） double-chain structure which is further connected through hydrogen bonding and π-π interactions into a three-dimensional （3D） supramolecular network. In addition, it exhibits blue fluorescence at room temperature in the solid state.
基金Supported by The National Institute of Dental and Craniofacial Research Grants,Nos.R01 DE022880 and K02 DE023551
文摘Persistent postsurgical pain is a serious issue in public health, which has received increased interest in recent years. Previous studies have reported that psychological factors promote the development of chronic postsurgical pain. However, it is unclear how chronification of postsurgical pain occurs. The α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptor(AMPA) phosphorylation in the central nervous system plays a critical role in synaptic plasticity and contributes to central sensitization and chronic pain development. Here, we discuss the role of AMPA receptor regulation in stress-induced pain chronification after surgery.
基金supported by Youth Backbone Teachers Project Funded by Xianyang Normal University(No.XSYGG201606)Scientific Research Program Funded by Shaanxi Provincial Education Department(No.16JK1822)+3 种基金Natural Science Basic Research Plan Funded by Shaanxi Province of China(No.2016JM5024)Science and Technology Projects of Xianyang City(No.2017k02-19)University Students Research and Innovation Training Program of Xianyang Normal University(No.2017060&201710722003)University Students Research and Innovation Training Program of Shaanxi Province(No.2490)
文摘The reaction of 5-hydroxyl-7-methoxyflavone（tectochrysin） with bromine obtained 3,6,8-tribromo-5-hydroxy-2,7-dimethoxy-2,3-dihydrochromen-4-one（1）, which was characterized by FT-IR, 1 H-NMR, 13C-NMR, elemental analysis and X-ray single-crystal diffraction. Complex 1 belongs to the monoclinic system, space group pbca with a = 9.4673（8）, b = 17.9938（15）, c = 21.2004（17） A, V = 3611.5（5） A3, Z = 8, μ = 0.6726 mm^（-1）, Dc = 1.795 g/cm3, F（000） = 2080, the final R = 0.0358 and wR = 0.0644 with I 2σ（I）. The results show that the addition reaction occurs at the carbon-carbon double bond（C2 and C3） of tectochrysin and 1 belongs to dihydroflavone. The reaction mechanism was discussed and the structure revealed that the crystal structure of 1 is stabilized by intramolecular hydrogen bonds and C–Br···π interactions. The antitumor ability of 1 was evaluated against human leukemia cells（K562）, human breast cancer cells（MCF-7） and human lung cancer cells（A549）. 1 exhibited potent antitumor activities against human leukemia cells（K562） with the IC50 values of 18.9 μmol/L.
