Fifteen novel 2-（3-oxobenzo[d]isothiazol-2（3H）-yl）ethyl benzoates were synthesi- zed by the condensation of 2-（2-hydroxyethyl）benzo[d]isothiazol-3（2H）-one with substituted benzoic acids in dichloromethane. All...Fifteen novel 2-（3-oxobenzo[d]isothiazol-2（3H）-yl）ethyl benzoates were synthesi- zed by the condensation of 2-（2-hydroxyethyl）benzo[d]isothiazol-3（2H）-one with substituted benzoic acids in dichloromethane. All the compounds were characterized by elemental analysis, IR, ESI-MS and 1H NMR. The crystal structures for 2-（2-hydroxyethyl）benzo[d]isothiazol-3（2H）-one （2） and 2-（3-oxobenzo[d]isothiazol-2（3H）-yl）ethyl 2-methoxybenzoate （30） have been determined by X-ray crystal structure analysis. Compound 2 （C9H9NO2S） crystallizes in the monoclinic system, space group Pn with a = 10.552（3）, b = 7.849（2）, c = 10.765（4） A, β = 103.128（4）°, V= 868.3（5） A3, Mr = 195.24, Dc = 1.493 Mg.m-3, μ = 0.33 mm-1, F（000） = 408, Z = 4, R= 0.0314 and wR= 0.0628. Compound 30 （C17H15NO4S） crystallizes in the triclinic system, space group P1 with a = 8.028（2）, b = 9.300（2）, c = 10.430（3）A, V= 752.1（3）A3, Mr = 329.36, D,= 1.454 Mg.m-3, p = 0.24 mm-1, F（000） = 344, Z = 2, R = 0.0377 and wR = 0.0904. The preliminary biological test indicated that the title compounds show better growth inhibitory activity against the gram-positive bacteria than the gram-negative bacteria.展开更多
Eighteen 2′,4′-difluoro-3-（carbamoyl）biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analys...Eighteen 2′,4′-difluoro-3-（carbamoyl）biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.展开更多
Two new one-dimensional chains extended by alternate benzenedicarboxylate（BDC） and 4-（2,6-di（pyrazin-2-yl）pyridin-4-yl）benzoate（L-） connectors, {[Cu（L）（BDC）（0.5）]·3.5 H2 O}n （1） and {[Zn（L）（BD...Two new one-dimensional chains extended by alternate benzenedicarboxylate（BDC） and 4-（2,6-di（pyrazin-2-yl）pyridin-4-yl）benzoate（L-） connectors, {[Cu（L）（BDC）（0.5）]·3.5 H2 O}n （1） and {[Zn（L）（BDC）（0.5）] ·H2 O}n （2）, were solvothermally synthesized. Complex 1 is in triclinic system, space group P1 with a = 9.6456（14）, b = 11.1160（16）, c = 12.0414（18） A, α = 106.266（3）, β = 92.277（3）, γ =108.104（3）°, V = 1166.6（3） A3, Dc = 1.603 g·cm（-3）, Mr = 563.00, Z = 2, F（000） = 578, μ = 0.996 mm（-1）, the final R = 0.0575 and wR = 0.1386 for 3704 observed reflections with I ＆gt; 2σ（I）. Complex 2 crystallizes in monoclinic, space group C2/c with a = 28.607（5）, b = 8.9767（16）, c = 19.705（4） ？, β = 125.396（3）°, V = 4125.0（13） ？3, Dc = 1.674 g·cm（-3）, Mr = 519.79, Z = 8, F（000） = 2120, μ = 1.242 mm（-1）, the final R = 0.0487 and w R = 0.0907 for 2944 observed reflections with I ＆gt; 2σ（I）. Resulting from the narrower band gap and broader response to visible light, the CuII-chain exhibits better photocatalytic performance towards the degradation of rhodamine B and methylene blue than those of ZnII-chain.展开更多
The title compound tert-butyl 4-[（E）-4-（1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl）- 1-butenyl] benzoate has been synthesized and characterized by X-ray crystallography. It crystallizes in monoclinic, space group C2/c...The title compound tert-butyl 4-[（E）-4-（1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl）- 1-butenyl] benzoate has been synthesized and characterized by X-ray crystallography. It crystallizes in monoclinic, space group C2/c with a = 14.875（3）, b = 8.9796（13）, c = 34.736（6） A°, β = 95.981（4）°, V= 4614.4（14）A°^3, Z= 8, Dc = 1.213 g/cm^3, F（000） = 1792,μ（MoKα） = 0.084 mm^-1, R = 0.0602 and wR = 0.1445 for 4613 unique reflections with 2272 observed ones （I〉 2σ（I））. The results of crystal structure determination show that the title compound has a layer structure, and the two benzene rings in molecule are parallel to each other.展开更多
Dual fluorescence and UV absorption of 2′-ethylhexyl 4-（N,N-dimethylamino）benzoate （EHDMAB） were investigated in cationic, non-ionic and anionic micelles. When EHDMAB was solubilized in different micelles, the UV...Dual fluorescence and UV absorption of 2′-ethylhexyl 4-（N,N-dimethylamino）benzoate （EHDMAB） were investigated in cationic, non-ionic and anionic micelles. When EHDMAB was solubilized in different micelles, the UV absorption of EHDMAB was enhanced. Twisted intramolecular charge transfer （TICT） emission with longer wavelength was observed in ionic micelles, whereas TICT emission with shorter wavelength was obtained in non-ionic micelles. In particular, dual fluorescence of EHDMAB was significantly quenched by the positively charged pyridinium ions arranged in the Stern layer of cationic micelles. UV radiation absorbed mainly decays via TICT emission and radiationless deactivation. The dimethylamino group of EHDMAB experiences different polar environments in ionic and non-ionic micelles according to the polarity dependence of TICT emission of EHDMAB in organic solvents. In terms of the molecular structures and sizes of EHDMAB and surfactants, each individual EHDMAB molecule should be buried in micelles with its dimethylamino group toward the polar head groups of different micelles and with its 2′-ethylhexyl chain toward the hydrophobic micellar core. Dynamic fluorescence quenching measurements of EHDMAB provide further support for the location of EHDMAB in different micelles.展开更多
OBJECTIVE To study the protective effect of potassium 2-(l-hydroxypentyl)-benzoate(PHPB) on hippocampal neurons,synapses and dystrophic axons in APP/PS1 mice.METHODS Ten-month-old male APP/PS1 transgenic mice and age-...OBJECTIVE To study the protective effect of potassium 2-(l-hydroxypentyl)-benzoate(PHPB) on hippocampal neurons,synapses and dystrophic axons in APP/PS1 mice.METHODS Ten-month-old male APP/PS1 transgenic mice and age-matched wild-type mice were randomly divided into three groups:wild-type group(WT Con group,n=10),APP/PS1 group(Tg Con group,n=10) and PHPB treated APP/PS1 group(PHPB group,n=10).PHPB group received 30 mg · kg-1 PHPB by oral gavage once daily for 3 months.WT Con group and Tg Con group received the same volume of water.Three months later,mice were sacrificed for biochemical and pathological testing such as transmission electron microscopy,Golgi staining and Western boltting analysis.RESULTS Under the transmission electron microscope,most hippocampal neurons and subcel ular organel es in WT Con group exhibited normal morphology.However,the degenerative changes were observed in Tg Con group such as nuclear fragmentation,mitochondrial swelling,ribosomes detachment and autophagic vacuoles accumulation.The hippocampal synapses number and the thickness of postsynaptic density(PSD) were significantly decreased in Tg Con group compared with the WT Con group(P<0.05).After PHPB treatment,the degenerative changes in APP/PS1 mice were alleviated to some extent.The synapse number has been elevated significantly(P<0.05) and the PSD has been thickened as well.Golgi staining showed that the spine density of secondary and tertiary apical dendritic branches was significantly decreased in CA1 and DG areas of Tg Con group(P<0.05).Sholl analysis revealed a decrease of dendritic complexity in Tg Con group compared with WT Con group(P<0.05).These abnormalities were alleviated to some extent after PHPB treatment.Western blotting study showed that the protein levels of synaptic marker PSD-95 and synaptophysin were significantly decreased in the hippocampus of Tg Con group(P<0.05).A significant increase of PSD-95(P<0.05) and a slight increase of SYP were observed after the PHPB treatment.Besides,we found a significant increase in the ratio of LC3-Ⅱ/LC3-Ⅰ in Tg Con group compared with the WT Con group(P<0.01) and the relevant improvement after PHPB treatment(P<0.05),which showed the regulatory effect of PHPB on autophagy impairment.CONCLUSION PHPB showed protective effects on hippocampal neurons,synapses and dystrophic axons in APP/PS1 mice,which might help explain its role on cognitive improvement in Alzheimer disease treatment.展开更多
目的:通过对比二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮与二甲双胍、盐酸吡格列酮联合阿卡波糖治疗2型糖尿病的临床效果,分析二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗2型糖尿病的临床应用价值。方法:选取2013年6月-2015年1月在...目的:通过对比二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮与二甲双胍、盐酸吡格列酮联合阿卡波糖治疗2型糖尿病的临床效果,分析二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗2型糖尿病的临床应用价值。方法:选取2013年6月-2015年1月在笔者所在医院住院治疗的2型糖尿病患者52例作为研究对象。随机分为两组,对照组患者采取二甲双胍、盐酸吡格列酮联合阿卡波糖治疗;试验组患者采取二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗。结果:试验组患者的临床总有效率为96.0%,对照组患者的临床总有效率为80.0%,两组患者的临床总有效率比较差异有统计学意义(P<0.05)。两组患者治疗前空腹血糖(FPG)、餐后2 h血糖(2 h PG)、体质指数(BMI)及糖化血红蛋白(Hb A1c)相比差异无统计学意义(P>0.05);治疗后空腹血糖(FPG)、餐后2 h血糖(2 h PG)、体质指数(BMI)及糖化血红蛋白(Hb A1c)相比差异均有统计学意义(P<0.05);治疗前后两组患者各项血糖指标相比差异均有统计学意义(P<0.05)。结论:二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗2型糖尿病通过降低肝糖生成、改善胰岛素敏感性以及升高体内胰升糖素样肽-1的浓度并恢复其刺激胰岛素分泌的作用等途径来控制血糖,疗效显著,具有一定的临床应用价值。展开更多
基金Supported by the National Natural Science Foundation of China (No. 20962007)
文摘Fifteen novel 2-（3-oxobenzo[d]isothiazol-2（3H）-yl）ethyl benzoates were synthesi- zed by the condensation of 2-（2-hydroxyethyl）benzo[d]isothiazol-3（2H）-one with substituted benzoic acids in dichloromethane. All the compounds were characterized by elemental analysis, IR, ESI-MS and 1H NMR. The crystal structures for 2-（2-hydroxyethyl）benzo[d]isothiazol-3（2H）-one （2） and 2-（3-oxobenzo[d]isothiazol-2（3H）-yl）ethyl 2-methoxybenzoate （30） have been determined by X-ray crystal structure analysis. Compound 2 （C9H9NO2S） crystallizes in the monoclinic system, space group Pn with a = 10.552（3）, b = 7.849（2）, c = 10.765（4） A, β = 103.128（4）°, V= 868.3（5） A3, Mr = 195.24, Dc = 1.493 Mg.m-3, μ = 0.33 mm-1, F（000） = 408, Z = 4, R= 0.0314 and wR= 0.0628. Compound 30 （C17H15NO4S） crystallizes in the triclinic system, space group P1 with a = 8.028（2）, b = 9.300（2）, c = 10.430（3）A, V= 752.1（3）A3, Mr = 329.36, D,= 1.454 Mg.m-3, p = 0.24 mm-1, F（000） = 344, Z = 2, R = 0.0377 and wR = 0.0904. The preliminary biological test indicated that the title compounds show better growth inhibitory activity against the gram-positive bacteria than the gram-negative bacteria.
基金the Opening Foundation of The Biochemical Engineering Key Discipline (No.20050105) Zhejiang,China,for financial supportthe National Center for Drug Screening,Shanghai,China,for evaluation of anti-inflammatory and analgesic activity.
文摘Eighteen 2′,4′-difluoro-3-（carbamoyl）biphenyl-4-yl benzoates were synthesized from diflunisal in three steps with total yields from 72% to 86%. All compounds were identified by IR, 1^H NMR, MS and elemental analysis. The anti-inflammatory activity and analgesic activity for 18 compounds were evaluated. The preliminary assay results showed that compounds 4a and 4p exhibited potent anti-inflammatory-analgesic activity.
文摘Two new one-dimensional chains extended by alternate benzenedicarboxylate（BDC） and 4-（2,6-di（pyrazin-2-yl）pyridin-4-yl）benzoate（L-） connectors, {[Cu（L）（BDC）（0.5）]·3.5 H2 O}n （1） and {[Zn（L）（BDC）（0.5）] ·H2 O}n （2）, were solvothermally synthesized. Complex 1 is in triclinic system, space group P1 with a = 9.6456（14）, b = 11.1160（16）, c = 12.0414（18） A, α = 106.266（3）, β = 92.277（3）, γ =108.104（3）°, V = 1166.6（3） A3, Dc = 1.603 g·cm（-3）, Mr = 563.00, Z = 2, F（000） = 578, μ = 0.996 mm（-1）, the final R = 0.0575 and wR = 0.1386 for 3704 observed reflections with I ＆gt; 2σ（I）. Complex 2 crystallizes in monoclinic, space group C2/c with a = 28.607（5）, b = 8.9767（16）, c = 19.705（4） ？, β = 125.396（3）°, V = 4125.0（13） ？3, Dc = 1.674 g·cm（-3）, Mr = 519.79, Z = 8, F（000） = 2120, μ = 1.242 mm（-1）, the final R = 0.0487 and w R = 0.0907 for 2944 observed reflections with I ＆gt; 2σ（I）. Resulting from the narrower band gap and broader response to visible light, the CuII-chain exhibits better photocatalytic performance towards the degradation of rhodamine B and methylene blue than those of ZnII-chain.
文摘The title compound tert-butyl 4-[（E）-4-（1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl）- 1-butenyl] benzoate has been synthesized and characterized by X-ray crystallography. It crystallizes in monoclinic, space group C2/c with a = 14.875（3）, b = 8.9796（13）, c = 34.736（6） A°, β = 95.981（4）°, V= 4614.4（14）A°^3, Z= 8, Dc = 1.213 g/cm^3, F（000） = 1792,μ（MoKα） = 0.084 mm^-1, R = 0.0602 and wR = 0.1445 for 4613 unique reflections with 2272 observed ones （I〉 2σ（I））. The results of crystal structure determination show that the title compound has a layer structure, and the two benzene rings in molecule are parallel to each other.
基金This work was supported by the National Natural Science Foundation of China （No.20335030） and the Innovation Foundation of Science and Technology （No.NWNU-KJCXGC-02-09）.
文摘Dual fluorescence and UV absorption of 2′-ethylhexyl 4-（N,N-dimethylamino）benzoate （EHDMAB） were investigated in cationic, non-ionic and anionic micelles. When EHDMAB was solubilized in different micelles, the UV absorption of EHDMAB was enhanced. Twisted intramolecular charge transfer （TICT） emission with longer wavelength was observed in ionic micelles, whereas TICT emission with shorter wavelength was obtained in non-ionic micelles. In particular, dual fluorescence of EHDMAB was significantly quenched by the positively charged pyridinium ions arranged in the Stern layer of cationic micelles. UV radiation absorbed mainly decays via TICT emission and radiationless deactivation. The dimethylamino group of EHDMAB experiences different polar environments in ionic and non-ionic micelles according to the polarity dependence of TICT emission of EHDMAB in organic solvents. In terms of the molecular structures and sizes of EHDMAB and surfactants, each individual EHDMAB molecule should be buried in micelles with its dimethylamino group toward the polar head groups of different micelles and with its 2′-ethylhexyl chain toward the hydrophobic micellar core. Dynamic fluorescence quenching measurements of EHDMAB provide further support for the location of EHDMAB in different micelles.
基金National Natural Sciences Foundation of China(8147320081673420)CAMS InnovationFund for Medical Sciences (2017-I2M-2-004).
文摘OBJECTIVE To study the protective effect of potassium 2-(l-hydroxypentyl)-benzoate(PHPB) on hippocampal neurons,synapses and dystrophic axons in APP/PS1 mice.METHODS Ten-month-old male APP/PS1 transgenic mice and age-matched wild-type mice were randomly divided into three groups:wild-type group(WT Con group,n=10),APP/PS1 group(Tg Con group,n=10) and PHPB treated APP/PS1 group(PHPB group,n=10).PHPB group received 30 mg · kg-1 PHPB by oral gavage once daily for 3 months.WT Con group and Tg Con group received the same volume of water.Three months later,mice were sacrificed for biochemical and pathological testing such as transmission electron microscopy,Golgi staining and Western boltting analysis.RESULTS Under the transmission electron microscope,most hippocampal neurons and subcel ular organel es in WT Con group exhibited normal morphology.However,the degenerative changes were observed in Tg Con group such as nuclear fragmentation,mitochondrial swelling,ribosomes detachment and autophagic vacuoles accumulation.The hippocampal synapses number and the thickness of postsynaptic density(PSD) were significantly decreased in Tg Con group compared with the WT Con group(P<0.05).After PHPB treatment,the degenerative changes in APP/PS1 mice were alleviated to some extent.The synapse number has been elevated significantly(P<0.05) and the PSD has been thickened as well.Golgi staining showed that the spine density of secondary and tertiary apical dendritic branches was significantly decreased in CA1 and DG areas of Tg Con group(P<0.05).Sholl analysis revealed a decrease of dendritic complexity in Tg Con group compared with WT Con group(P<0.05).These abnormalities were alleviated to some extent after PHPB treatment.Western blotting study showed that the protein levels of synaptic marker PSD-95 and synaptophysin were significantly decreased in the hippocampus of Tg Con group(P<0.05).A significant increase of PSD-95(P<0.05) and a slight increase of SYP were observed after the PHPB treatment.Besides,we found a significant increase in the ratio of LC3-Ⅱ/LC3-Ⅰ in Tg Con group compared with the WT Con group(P<0.01) and the relevant improvement after PHPB treatment(P<0.05),which showed the regulatory effect of PHPB on autophagy impairment.CONCLUSION PHPB showed protective effects on hippocampal neurons,synapses and dystrophic axons in APP/PS1 mice,which might help explain its role on cognitive improvement in Alzheimer disease treatment.
文摘目的:通过对比二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮与二甲双胍、盐酸吡格列酮联合阿卡波糖治疗2型糖尿病的临床效果,分析二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗2型糖尿病的临床应用价值。方法:选取2013年6月-2015年1月在笔者所在医院住院治疗的2型糖尿病患者52例作为研究对象。随机分为两组,对照组患者采取二甲双胍、盐酸吡格列酮联合阿卡波糖治疗;试验组患者采取二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗。结果:试验组患者的临床总有效率为96.0%,对照组患者的临床总有效率为80.0%,两组患者的临床总有效率比较差异有统计学意义(P<0.05)。两组患者治疗前空腹血糖(FPG)、餐后2 h血糖(2 h PG)、体质指数(BMI)及糖化血红蛋白(Hb A1c)相比差异无统计学意义(P>0.05);治疗后空腹血糖(FPG)、餐后2 h血糖(2 h PG)、体质指数(BMI)及糖化血红蛋白(Hb A1c)相比差异均有统计学意义(P<0.05);治疗前后两组患者各项血糖指标相比差异均有统计学意义(P<0.05)。结论:二甲双胍、苯甲酸阿格列汀联合盐酸吡格列酮治疗2型糖尿病通过降低肝糖生成、改善胰岛素敏感性以及升高体内胰升糖素样肽-1的浓度并恢复其刺激胰岛素分泌的作用等途径来控制血糖,疗效显著,具有一定的临床应用价值。
