3-(5-(2.4-dichlorophyenyl)-4.5-dihydro-1H-pyrazol-3-yl)-4hydroxy-1-methylquinolin(1H)-one, 5-((4-hydroxy-8-methyl-2-oxo-1.2-dihydroquinolin-3-yl)methylene)-1-phenyl-2-hioxodihydropyrimidine-4.6(1H.5H)-dione, and 1-but...3-(5-(2.4-dichlorophyenyl)-4.5-dihydro-1H-pyrazol-3-yl)-4hydroxy-1-methylquinolin(1H)-one, 5-((4-hydroxy-8-methyl-2-oxo-1.2-dihydroquinolin-3-yl)methylene)-1-phenyl-2-hioxodihydropyrimidine-4.6(1H.5H)-dione, and 1-butyl-4-hydroxy-3-(5-styryl-4.5-dihydro-1H-pyrazol-3yl)quinolin-2(1H)-one were synthesized and characterized by spectroscopy analysis. These compounds are designated I, II and III, respectively. The antioxidants efficiency of the synthesized compounds in lubricating greases had been investigated using ASTM d-942 and ASTM d-664. The obtained data showed that the total acid number and oxygen pressure drop of these compounds in lubricating greases decrease in the order: Comp.III. < Comp.I. < Comp.II. The antioxidant efficiency of the prepared quinolinones derivatives was discussed. Acceptable correlations were obtained between the obtained oxidation inhibition and the calculated quantum chemical parameters.展开更多
Six new N4-[bi-（4-fluorophenyl）-methyl]-piperazine thiosemicarbazones 3a-f have been prepared starting from [bi-（4-fluorophenyl）-methyl]-piperazine in solvent-free condition under microwave irradiation with excell...Six new N4-[bi-（4-fluorophenyl）-methyl]-piperazine thiosemicarbazones 3a-f have been prepared starting from [bi-（4-fluorophenyl）-methyl]-piperazine in solvent-free condition under microwave irradiation with excellent yields. Their structures have been determined by elemental analysis, IR, MS and 1H NMR data.展开更多
CC chemokine receptor 4(CCR4)is a kind of G-protein-coupled receptor,which plays a pivotal role in allergic inflammation.The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamlyl]-methyl-4-o...CC chemokine receptor 4(CCR4)is a kind of G-protein-coupled receptor,which plays a pivotal role in allergic inflammation.The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide(S009)and the N-terminal extracellular tail(ML40)of CCR4 has been validated to be high affinity by capillary zone electrophoresis(CZE).The S009 is a known CCR4 antagonist.Now,a series of new thiourea derivatives have been synthesized.Compared with positive control S009,they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation diseases.The synthesized compounds XJH-5,XJH-4,XJH-17 and XJH-1 displayed the interaction with ML40,but XJH-9,XJH-10,XJH-I 1,XJH-12,XJH-13,XJH-14,XJH-3,XJH-8,XJH-6,XJH-7,XJH-15,XJH-16 and XJH-2 did not bind to ML40.Both qualification and quantification characterizations of the binding were determined.The affinity of the four compounds was valued by the binding constant,which was similar with the results of chemotactic experiments.The established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.展开更多
The crystal structure of the title compound(E)-ethyl 2-(4-(2,4-dimethoxy benzylide-neamino)-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazol-3-ylthio)acetate(4,C_(24)H_(28)N_(4)O_(7)S,Mr=516.17)was synthesized and determin...The crystal structure of the title compound(E)-ethyl 2-(4-(2,4-dimethoxy benzylide-neamino)-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazol-3-ylthio)acetate(4,C_(24)H_(28)N_(4)O_(7)S,Mr=516.17)was synthesized and determined by X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group P2_(1)/n with a=13.162(2),b=8.4506(13),c=22.602(4)Å,β=99.888(3)°,μ=0.183 mm^(-1),V=2476.5(7)Å^(3),Z=4,D_(c)=1.385 g/cm^(3),F(000)=1088,T=110(2)K,R=0.0426 and wR=0.1216 for 3859 observed reflections with I 2σ(Ⅰ).展开更多
Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide d...Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide derivatives were synthesised for studying their biological activities especially cardiovascular activity.Their chemical structures were confirmed by 1 H NMR,MS and IR.The preliminary tests with isolated heart of rabbits indicated that both mixtures,A 1B 1,A 2B 2,had more positive inotropic effect than vesnarinone which appeared on the market in Japanese.The results of the pharmacological tests showed that the two mixtures did not affect the blood pressure and respiration of the dogs.展开更多
31 samples of shales and mudstones developed in reducing hypersaline andfreshwater setting and 20 oil samples of Bamianhe oilfield, Bohai Bay basin were collected for adetailed study of petroleum system. Composition a...31 samples of shales and mudstones developed in reducing hypersaline andfreshwater setting and 20 oil samples of Bamianhe oilfield, Bohai Bay basin were collected for adetailed study of petroleum system. Composition and distribution, especially significance ofsteroids, are discussed as a part of those. Abundant steroidal biomarkers, including C_(27-29)regular Steranes, C_(28-30) 4-methyl steranes, di-nosteranes and aromatic steranes, were detected.Results show that the composition and distribution of the steroids in samples studied are functionsof thermal maturity, organic source, paleoenvironment and lithology of potential source rocks.Alga-rich Es_4 shales (brackish water) developed in the south slope of depocenter (Niuzhuang sag)were found particularly rich in steroidal biomarkers including C_(30) 4-methyl steranes anddinosteranes. Es_3 mudstones (fresh water) were found devoid of dinosteranes. Distribution patternsof regular steranes are completely different from methyl steranes indicating different origins ofthe specific compounds of the fractioa Diagnostic distribution of steranes in rock extracts ofdiverse intervals makes the compounds to be essential indictors of source-rock tracing. Methylsteranes prove to be much more useful in oil-source rock correlation than regular steranes. Resultsalso show that alga-rich Es_4 shales located in the south slope are not likely the primary sourcerock responsible for the oils discovered based on the composition and distribution of steroids.展开更多
文摘3-(5-(2.4-dichlorophyenyl)-4.5-dihydro-1H-pyrazol-3-yl)-4hydroxy-1-methylquinolin(1H)-one, 5-((4-hydroxy-8-methyl-2-oxo-1.2-dihydroquinolin-3-yl)methylene)-1-phenyl-2-hioxodihydropyrimidine-4.6(1H.5H)-dione, and 1-butyl-4-hydroxy-3-(5-styryl-4.5-dihydro-1H-pyrazol-3yl)quinolin-2(1H)-one were synthesized and characterized by spectroscopy analysis. These compounds are designated I, II and III, respectively. The antioxidants efficiency of the synthesized compounds in lubricating greases had been investigated using ASTM d-942 and ASTM d-664. The obtained data showed that the total acid number and oxygen pressure drop of these compounds in lubricating greases decrease in the order: Comp.III. < Comp.I. < Comp.II. The antioxidant efficiency of the prepared quinolinones derivatives was discussed. Acceptable correlations were obtained between the obtained oxidation inhibition and the calculated quantum chemical parameters.
基金Natural Foundation of Southwest University for Nationalities(No.234688).
文摘Six new N4-[bi-（4-fluorophenyl）-methyl]-piperazine thiosemicarbazones 3a-f have been prepared starting from [bi-（4-fluorophenyl）-methyl]-piperazine in solvent-free condition under microwave irradiation with excellent yields. Their structures have been determined by elemental analysis, IR, MS and 1H NMR data.
基金supported by the National Key New Drug Creation Program of China(2009ZX09103-724)the National Natural Science Foundation of China grants(30872292,90813025 and 81072612)+2 种基金the Natural Science Foundation of Beijing(7102107)the Open Foundation of State Key Laboratory of Natural and Biomimetic Drugs(K20090207)the National New Drug Research and Development Project of China(2009ZX09301-010)
文摘CC chemokine receptor 4(CCR4)is a kind of G-protein-coupled receptor,which plays a pivotal role in allergic inflammation.The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide(S009)and the N-terminal extracellular tail(ML40)of CCR4 has been validated to be high affinity by capillary zone electrophoresis(CZE).The S009 is a known CCR4 antagonist.Now,a series of new thiourea derivatives have been synthesized.Compared with positive control S009,they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation diseases.The synthesized compounds XJH-5,XJH-4,XJH-17 and XJH-1 displayed the interaction with ML40,but XJH-9,XJH-10,XJH-I 1,XJH-12,XJH-13,XJH-14,XJH-3,XJH-8,XJH-6,XJH-7,XJH-15,XJH-16 and XJH-2 did not bind to ML40.Both qualification and quantification characterizations of the binding were determined.The affinity of the four compounds was valued by the binding constant,which was similar with the results of chemotactic experiments.The established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.
基金supported by the Science Foundation of the Southern Medical University for New Excellent Talents(No.B1000374)the Natural Science Foundation of Guangdong Province(No.10451051501004725)
文摘The crystal structure of the title compound(E)-ethyl 2-(4-(2,4-dimethoxy benzylide-neamino)-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazol-3-ylthio)acetate(4,C_(24)H_(28)N_(4)O_(7)S,Mr=516.17)was synthesized and determined by X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group P2_(1)/n with a=13.162(2),b=8.4506(13),c=22.602(4)Å,β=99.888(3)°,μ=0.183 mm^(-1),V=2476.5(7)Å^(3),Z=4,D_(c)=1.385 g/cm^(3),F(000)=1088,T=110(2)K,R=0.0426 and wR=0.1216 for 3859 observed reflections with I 2σ(Ⅰ).
文摘Isoflavonoids possess broad activities besides cardiovascular activity.3 phenyl 4(1H)quinolinone derivatives are isosteres of isoflavonoids.They have similar spatial structures.Eight 3 phenyl 4(1H)quinolinone halide derivatives were synthesised for studying their biological activities especially cardiovascular activity.Their chemical structures were confirmed by 1 H NMR,MS and IR.The preliminary tests with isolated heart of rabbits indicated that both mixtures,A 1B 1,A 2B 2,had more positive inotropic effect than vesnarinone which appeared on the market in Japanese.The results of the pharmacological tests showed that the two mixtures did not affect the blood pressure and respiration of the dogs.
基金ThispaperissupportedbytheNaturalScienceResearchCouncilofChi na (underChina 973NationalKeyResearchandDevelopmentProgram #G1 999 4331 0 ) .
文摘31 samples of shales and mudstones developed in reducing hypersaline andfreshwater setting and 20 oil samples of Bamianhe oilfield, Bohai Bay basin were collected for adetailed study of petroleum system. Composition and distribution, especially significance ofsteroids, are discussed as a part of those. Abundant steroidal biomarkers, including C_(27-29)regular Steranes, C_(28-30) 4-methyl steranes, di-nosteranes and aromatic steranes, were detected.Results show that the composition and distribution of the steroids in samples studied are functionsof thermal maturity, organic source, paleoenvironment and lithology of potential source rocks.Alga-rich Es_4 shales (brackish water) developed in the south slope of depocenter (Niuzhuang sag)were found particularly rich in steroidal biomarkers including C_(30) 4-methyl steranes anddinosteranes. Es_3 mudstones (fresh water) were found devoid of dinosteranes. Distribution patternsof regular steranes are completely different from methyl steranes indicating different origins ofthe specific compounds of the fractioa Diagnostic distribution of steranes in rock extracts ofdiverse intervals makes the compounds to be essential indictors of source-rock tracing. Methylsteranes prove to be much more useful in oil-source rock correlation than regular steranes. Resultsalso show that alga-rich Es_4 shales located in the south slope are not likely the primary sourcerock responsible for the oils discovered based on the composition and distribution of steroids.
