期刊文献+
共找到50篇文章
< 1 2 3 >
每页显示 20 50 100
Synthesis, Structural Characterization and Antimicrobial Activity of a Novel Cobalt(II) Complex Based on 3-Methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
1
作者 Emeline Sorelle Mefouegang Claudelle Sybilline Anensong Djadock +5 位作者 Golngar Djimassingar Gabriel Tchuente Kamsu Donald Raoul Tchuifon Tchuifon Alain Charly Tagne Kuate Dirk Bockfeld Jean Ngoune 《Journal of Materials Science and Chemical Engineering》 2023年第8期109-126,共18页
New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<s... New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus). 展开更多
关键词 COBALT ACYLPYRAZOLONE X-Ray Diffraction Antimicrobial Activity 3-methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
下载PDF
Synthesis, Structural Characterization and Antimicrobial Activity of a Novel Cobalt(II) Complex Based on 3-Methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
2
作者 Emeline Sorelle Mefouegang Claudelle Sybilline Anensong Djadock +5 位作者 Golngar Djimassingar Gabriel Tchuente Kamsu Donald Raoul Tchuifon Tchuifon Alain Charly Tagne Kuate Dirk Bockfeld Jean Ngoune 《Journal of Modern Physics》 2023年第8期109-126,共12页
New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<s... New cobalt(II) complex, [Co(O<sub>2</sub>C<sub>15</sub>H<sub>11</sub>N<sub>2</sub>S)<sub>2</sub>(OH<sub>2</sub>)<sub>2</sub>]∙2H<sub>2</sub>O (1∙2H<sub>2</sub>O), has been synthesized upon reaction of cobalt chloride hexahydrate (Co(Cl)<sub>2</sub>∙6H<sub>2</sub>O) with 3-methyl-1-Phenyl-4-(2-thienoyl)-pyrazol-5-one (referred as HL) in ethanol at room temperature. Single crystal X-ray diffraction (XRD), spectroscopic methods, and microelemental analyses were used to characterize 1∙2H<sub>2</sub>O. Compound 1∙2H<sub>2</sub>O crystallizes in the orthorhombic crystal system with a Pbca space group and with the cobalt atom being pseudo-octahedral coordinated. The broth microdilution technique was used to screen the free ligand (HL) and the complex (1∙2H<sub>2</sub>O) for antimicrobial activities. HL has a low activity (MIC > 100 μg/mL) on all microorganisms, whereas compound 1∙2H<sub>2</sub>O displayed moderate activity (10 ∙2H<sub>2</sub>O exhibited bactericidal and fungicidal activity respectively on all the bacteria and yeasts tested. These findings reveal that the antimicrobial activity of HL was enhanced upon coordination to Co(II) ion against all microorganisms (bacteria and fungus). 展开更多
关键词 COBALT ACYLPYRAZOLONE X-Ray Diffraction Antimicrobial Activity 3-methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
下载PDF
Novel synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde:A key intermediate of Losartan 被引量:3
3
作者 Hai Bo Sun Guo Jun Zheng +2 位作者 Ya Ping Wang Xiang Jing Wang Wen Sheng Xiang 《Chinese Chemical Letters》 SCIE CAS CSCD 2009年第3期269-270,共2页
A novel method for synthesis of 2-butyl-5 -chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized from starting material dimethyl malonate 6 and n-valeronitri... A novel method for synthesis of 2-butyl-5 -chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized from starting material dimethyl malonate 6 and n-valeronitrile 8 by six steps with an overall yield of 40%. The key step including the reaction of compound 5 with POCl3/DMF followed by hydrolysis to give compound 2 with the yield of 68%. 展开更多
关键词 LOSARTAN ANTIHYPERTENSIVE Angiotensin II 2-Butyl-5-chloro-3H-imidazole-4-carbaldehyde
下载PDF
Synthesis, Crystal Structure and Antitumor Activity of 2-(3-Methyl-5-(methylthio)-4H-1,2,4-triazol-4-yl)isoindoline-1,3-dione 被引量:6
4
作者 赵培亮 胡孟金 +2 位作者 段安娜 孙晓敏 游文玮 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2015年第3期359-364,共6页
The title compound 2-(3-methyl-5-(methylthio)-4H-1,2,4-triazol-4-yl)isoindoline- 1,3-dione (C12H10NaO2S, Mr= 274.30) has been synthesized by a three-step procedure including the cyclization, hydrazinolysis and s... The title compound 2-(3-methyl-5-(methylthio)-4H-1,2,4-triazol-4-yl)isoindoline- 1,3-dione (C12H10NaO2S, Mr= 274.30) has been synthesized by a three-step procedure including the cyclization, hydrazinolysis and substitution reactions, and its crystal structure was determined by X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P2/c with a = 12.264(3), b = 14.646(3), c = 14.349(4) A,β = 91.69(3)°,μ = 0.255 mm1, Mr = 274.30, V = 2576.2(10) A3, Z =8, Dc = 1.414 g/cm3, F(000) = 1136, R = 0.0487 and wR = 0.1329 for 4048 observed reflections with I 〉 2σ(I). In addition, the preliminary bioassay suggested that the title compound 6 exhibits relatively good antitumor activity against HT-29 and MCF-7. 展开更多
关键词 2-(3-methyl-5-(methylthio)-4H-1 2 4-triazol-4-yl)isoindoline-l 3-dione synthesis
下载PDF
Differential protein expression in substantia nigra induced by 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine in a mouse model of chronic Parkinson’s disease 被引量:2
5
作者 Wenbin Tu Furong Xu Guoguang Peng 《Neural Regeneration Research》 SCIE CAS CSCD 2008年第5期482-485,共4页
BACKGROUND: To date, a complete protein expression profile of the midbrain substantia nigra in a mouse model of chronic Parkinson's disease, induced by 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP), does ... BACKGROUND: To date, a complete protein expression profile of the midbrain substantia nigra in a mouse model of chronic Parkinson's disease, induced by 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP), does not exist. In addition, there are no reports of analysis of differential protein expression. OBJECTIVE: To separate and evaluate MPTP-induced differential protein expression through the use of proteomics in the substantia nigra of a mouse model of chronic Parkinson's disease. DESIGN: Randomized controlled animal study. SETTING: Department of Neurology, the First Affiliated Hospital, Chongqing Medical University. MATERIALS: Sixteen 8-10-week old, healthy, male, C57BL mice, weighing 20-25 g, and of clean grade, were provided by the Experimental Animal Center of Chongqing Medical University. The experimental animals were disposed according to ethical criteria. MPTP was provided by Sigma Company, USA; Pdquest 2D image analysis software and gelatum/irradiance image analysis system (ChemiDoc XRS) by Bio-Rad, USA; and Voyager DE-PROMALD1-TOF-MS mass spectroscopy analyzer by AB1 Company, USA. METHODS: This study was performed in Chongqing Neurological Laboratory between November 2006 and July 2007. Mice were randomly divided into model and control groups, with 8 mice in each group. Mice in the model group were received a subcutaneous injection of MPTP (25 mg&g), twice a week, for five successive weeks, to establish a chronic Parkinson's disease model. Mice in the control group received the same volume of a subcutaneous saline injection at the same time points. Mice were sacrificed by anesthesia to rapidly obtain the midbrain for protein separation of the substantia nigra. MAIN OUTCOME MEASURES: (1) 2-ED handbook (Bio-Rad Company) was referenced for two-dimensional electrophoresis, (2) PDQUEST8,0 analytical electrophoresis pattern was adopted to evaluate differential protein expression. (3) Peptide mass finger print map and data were retrieved on http://www.prospector.ucsf.edu to compare differential substantia nigral protein expression in the two groups. RESULTS: Two-dimensional gel electrophoresis of substantia nigra tissue indicated that there were 33 differential protein expressions between the two groups. Three new proteins were evaluated, including α -enolase, which exhibited regulated expression, tumor necrosis factor ligand superfamily member 4, and cyclin-dependent kinase inhibitor 1B. CONCLUSION: There are three proteins that exhibit differential expression in the substantia nigra- α -enolase, tumor necrosis factor ligand superfamily member 4, and cyclin-dependent kinase inhibitor 1B. 展开更多
关键词 Parkinson's disease 1-methyl-4-phenyl-l 2 3 6-tetrahydropyridine mice substantia nigra proteomics
下载PDF
Synthesis of fused pyran and arylbis(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)methane in ionic liquid 被引量:2
6
作者 Xue Sen Fan Ying Ying Qu Xin Ying Zhang Xia Wang Jian Ji Wang 《Chinese Chemical Letters》 SCIE CAS CSCD 2009年第4期387-390,共4页
Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis(4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl)methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-... Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis(4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl)methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-methyl-2-oxo-pyran with or without acetic anhydride. By using these novel procedures, pyrimidine nucleoside-fused pyran and arylbis(pyranon-3-yl)methane hybrids with potential biological activities were constructed. 展开更多
关键词 Ionic liquid Fused pyran Arylbis(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)methane Pyrimidine nucleoside Green synthesis
下载PDF
Synthesis and Crystal Structure of Trans-4-[(5-(2,4-Dichlorophenoxy)-3-methyl-1-phenyl-1H-pyrazol-4-yl)methyleneamino]-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-one 被引量:4
7
作者 孙凤梅 田孟魁 +1 位作者 杨靖华 连照勋 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2008年第7期789-792,共4页
The title compound trans-4-[(5-(2,4-dichlorophenoxy)-3-methyl- 1-phenyl-1H-pyrazol-4-yl)methyleneamino]- 1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-one 3 (C28H23Cl2N5O2, Mr = 532.41) has been synthesized and its... The title compound trans-4-[(5-(2,4-dichlorophenoxy)-3-methyl- 1-phenyl-1H-pyrazol-4-yl)methyleneamino]- 1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-one 3 (C28H23Cl2N5O2, Mr = 532.41) has been synthesized and its crystal structure was determined by single-crystal X-ray diffraction analysis. It crystallizes in triclinic, space group P1- with a = 8.9438(4), b = 11.6065(5), c = 14.2215(6)A, α = 112.566(1), β = 92.324(2), γ = 102.91(1)°, V= 1315.65(10) A^3, Z = 2, Dc = 1.344 g/cm^3,μ(MoKa) = 0.282 mm^-1, λ = 0.71073 A, F(000) = 552, the final R = 0.0587 and wR = 0.1578 for 5071 observed reflections (I 〉 2σ(I)). X-ray analysis reveals that the product is a thermodynamically stable trans isomer. Intra- and intermolecular C( 12)-H(12)…O(1) and C(28)-H(28)...O(1)# 1 hydrogen bonds were observed in the title compound. 展开更多
关键词 trans-4-[ 5-(2 4-dichlorophenoxy)-3-methyl- 1-phenyl- 1H-pyrazol-4-yl)methylene amino]-1 5-dimethyl-2-phenyl-1 2-dihydropyrazol-3-one synthesis crystal structure
下载PDF
Synthesis and Crystal Structure of Ethyl 3-(4-Chlorophenyl)-3,4-dihydro-6-methyl-4-oxo-2-(pyrrolidin-1-yl)furo[2,3-d]pyrimidine-5-carboxylate 被引量:2
8
作者 胡扬根 徐靖 丁明武 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2009年第6期689-692,共4页
The crystal structure of the title compound ethyl 3-(4-chlorophenyl)-3,4-dihydro-6- methyl-4-oxo-2-(pyrrolidin-1-yl)furo[2,3-d]pyrimidine-5-carboxylate (C20H20ClN3O4, Mr= 401.84) has been prepared and determined... The crystal structure of the title compound ethyl 3-(4-chlorophenyl)-3,4-dihydro-6- methyl-4-oxo-2-(pyrrolidin-1-yl)furo[2,3-d]pyrimidine-5-carboxylate (C20H20ClN3O4, Mr= 401.84) has been prepared and determined by single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/n with a = 20.6215(9), b = 8.5311(4), c = 21.6886(9) A^°, β = 91.607(1)°, V = 3814.0(3)A^°^3, Z = 8, Dc = 1.400 g/cm^3, F(000) = 1680, μ = 0.233 mm^-1, R = 0.0718 and wR = 0.1545 for 6717 observed reflections with I 〉 2σ(I). X-ray diffraction analysis reveals two crystallographically independent molecules in the asymmetric unit. 展开更多
关键词 crystal structure ethyl 3-(4-ehlorophenyl)-3 4-dihydro-6-methyl-4-oxo-2- (pyrrolidin-1-yl)furo[2 3-d]pyrimidine-5-earboxylate aza-Wittig reaction synthesis
下载PDF
Synthesis and Crystal Structure of (Z)-Methyl-3-methoxy-2-{2-[(4-(E-3-p-tolylacryloyl)phenoxy)methyl]phenyl}acrylate 被引量:1
9
作者 周中振 游文玮 赵培亮 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第10期1574-1578,共5页
The title compound,(Z)-methyl-3-methoxy-2-{2-[(4-(E-3-p-tolylacryloyl)phenoxy)-methyl]phenyl}acrylate,was synthesized and determined by X-ray single-crystal diffraction. The crystal belongs to the triclinic syst... The title compound,(Z)-methyl-3-methoxy-2-{2-[(4-(E-3-p-tolylacryloyl)phenoxy)-methyl]phenyl}acrylate,was synthesized and determined by X-ray single-crystal diffraction. The crystal belongs to the triclinic system,space group P1 with a = 8.0157(8),b = 12.5748(13),c = 13.3768(14) ,α = 64.770(2),β = 75.720 (2),γ = 89.784(2)°,μ = 0.085 mm-1,Mr = 442.49,V = 1174.1(2) 3,Z = 2,Dc = 1.252 g/cm3,F(000) = 468,T = 294(2) K,R = 0.0603 and wR = 0.1498 for 2644 observed reflections with I 〉 2σ(I). X-ray diffraction analysis reveals that the single crystal contains strong non-classical hydrogen bonds. The preliminary bioassay showed that the title compound exhibits inhibitory activity against the Pseudoperoniospora cubensis and Rhizoctonia solani at the test concentration of 200 mg/L. 展开更多
关键词 synthesis crystal structure (Z)-methyl-3-methoxy-2-{2-[(4-(E-3-p-tolylacryloyl)phenoxy)methyl]phenyl}acrylate
下载PDF
Crystal Structure and Biological Activities of (R)-N′-[2-(4-Methoxy-6-chloro)-pyrimidinyl]-N-[3-methyl-2-(4-chlorophenyl)butyryl]-urea
10
作者 LI Jing-Zhi XUE Si-Jia LIU Guo-Hua 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2006年第8期903-908,共6页
The title compound (R)-N′-[2-(4-methoxy-6-chloro)-pyrimidyl]-N-[3-methyl-2-(4- chlorophenyl)butyryl]-urea has been synthesized, and its crystal structure and biological behaviors were studied. Crystallographic ... The title compound (R)-N′-[2-(4-methoxy-6-chloro)-pyrimidyl]-N-[3-methyl-2-(4- chlorophenyl)butyryl]-urea has been synthesized, and its crystal structure and biological behaviors were studied. Crystallographic data: C17H18C12N4O3, Mr = 397.25, monoclinic, space group P21/c, a = 12.331(2), b = 14.025(3), c = 23.085(5) A, β = 99.607(4)°, Z = 8, V = 3936.2(13) A3, Dc = 1.341 g/cm^3, F(000) = 1648, R = 0.0718, wR = 0.1585 and/t(MoKα) = 0.353 mm^-1. The preliminary biological tests showed that the title compound has definite insecticidal and fungicidal activities. 展开更多
关键词 crystal structure biological activity (R)-3-methyl-2-(4-chlorophenyl)butyric acid 2-amino-6-chloro-4-methoxy-pyrimidine
下载PDF
Two New Schiff Bases Based on 5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde: Syntheses, Crystal Structures and Properties
11
作者 SUN Feng-Mei HAN Qiong +4 位作者 JIANG Zheng-Jing ZHAO Pan-Xiang WANG Jia RUI Jia-Yi XU Ji-Ming 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2019年第3期408-415,共8页
Two new Schiff bases based on 5-chloro-3-methyl-1-phenyl-1 H-pyrazole-4-carbaldehyde, namely, N-((5-chloro-3-methyl-1-phenyl-1 H-pyrazol-4-yl)methylene)-4-morpholinoaniline(Ⅲa) and N-((5-chloro-3-methyl-1-phenyl-1 H-... Two new Schiff bases based on 5-chloro-3-methyl-1-phenyl-1 H-pyrazole-4-carbaldehyde, namely, N-((5-chloro-3-methyl-1-phenyl-1 H-pyrazol-4-yl)methylene)-4-morpholinoaniline(Ⅲa) and N-((5-chloro-3-methyl-1-phenyl-1 H-pyrazol-4-yl)methylene)-3-fluoro-4-morpholinoaniline(Ⅲb), were synthesized and characterized by IR, LC-MS, 1 H NMR and 13 C NMR spectroscopy. Meanwhile, the three-dimensional configurations of the two title compounds were further characterized by single-crystal X-ray diffraction analyses. Both the compounds are thermodynamically stable trans-isomers. Moreover, the fluorescence properties and antioxidant activities against DPPH of the two target compounds have been investigated, and the results showed that the title compounds both have fluorescence performance and certain antioxidant activities against DPPH radical. 展开更多
关键词 Schiff base 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde synthesis CRYSTAL structure property
下载PDF
Studies on the esterifications of 9-(hydroxyimino)-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one with acid chlorides under different conditions
12
作者 Ru Shu Sun Yang Wang Peng Xia 《Chinese Chemical Letters》 SCIE CAS CSCD 2008年第7期791-794,共4页
The esterifications of 9-(hydroxyimino)-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one (4) with acid chlorides afforded normal oxime-esters 3a-e in 35-78% yields in presence of excessive 4-dimethylaminopyridine as t... The esterifications of 9-(hydroxyimino)-4-methyl-8,9-dihydrofuro[2,3-h]chromen-2-one (4) with acid chlorides afforded normal oxime-esters 3a-e in 35-78% yields in presence of excessive 4-dimethylaminopyridine as the acid scavenger, whereas the reactions gave unexpected 8-substituted products N-(8-chloro-4-methyl-2-oxo-2H-furo-[2,3-h]chromen-9-yl)amides (5a-c) and 4-methyl-2,9-dioxo-8,9-dihydro-2H-furo[2,3-h]chromen-8-ylcarboxyloates (6d-e) by using excessive acid chlorides. The structures of 10 new compounds were determined by 1H NMR, 13C NMR, MS and HRMS, and the possible mechanism for the formation of unexpected products 5a--c and 6d-e was also proposed. 展开更多
关键词 9-(Hydroxyirnino)-4-methyl-8 9-dihydrofuro[2 3-h]chromen-2-one Oxime-ester N-(8-chloro-4-methyl-2-oxo-2H-furo[2 3-h]chro-men-9-yl)amide 4-methyl-2 9-dioxo-8 9-dihydro-2H-furo[2 3-h]chromen-8-ylcarboxyloate
下载PDF
Theoretical Study on the Structure and Vibrational Spectra for 4-methyl-3-penten-2-one
13
作者 Dong Mei DU Ai Ping FU Zheng Yu ZHOU (Department of Chemistry. Qufu Normal University, Shandong, Qufu 273165 2 State Key Laboratory of Crystal Materials. Shandong University, Shandong, Jinan 250100) 《Chinese Chemical Letters》 SCIE CAS CSCD 1999年第10期835-838,共4页
Density functional theory BLYP (using Becke's and Lee-Yang-Parr's correlation functionals), nb initio Hartree-Fock (HF) and hybrid DFT/HF B3LYP calculations were carried out to study the structure and vibratio... Density functional theory BLYP (using Becke's and Lee-Yang-Parr's correlation functionals), nb initio Hartree-Fock (HF) and hybrid DFT/HF B3LYP calculations were carried out to study the structure and vibrational spectra of 4-methyl-3-penten-2-one. The BLYP/6-31G* and scaled HF/6-31G* frequencies correspond well with each other and with available experimental assignment of the functional vibrational modes. 展开更多
关键词 density functional theory vibrational spectra 4-methyl-3-penten-2-one
下载PDF
Synthesis and Biological Activities of 2,4-Dichlorophenoxyacetyl(thio)urea and S-(+)-3-Methyl-2-(4-chlorophenyl)butyramide Derivatives
14
作者 LIU Li XUE Si-jia BU Hong-fei CHEN Long 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2010年第6期929-932,共4页
2,4-Dichlorophenoxyacetyl(thio)urea and S-(+)-3-methyl-2-(4-chlorophenyl)butyramides were synthesized via acylation,aminolysis,esterification and addition reactions,and the partial new compounds have desirable ... 2,4-Dichlorophenoxyacetyl(thio)urea and S-(+)-3-methyl-2-(4-chlorophenyl)butyramides were synthesized via acylation,aminolysis,esterification and addition reactions,and the partial new compounds have desirable bioactive activity. 展开更多
关键词 2 4-Dichlorophenoxyacetyl(thio)urea S-(+)-3-methyl-2-(4-chlorophenyl)butyramide Herbicidal activity Fungicidal activity
下载PDF
Establishing motor disorder mouse models of Parkinson disease Comparison of 6-hydroxydompamine and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine
15
作者 Zhi hua Ren Jie Gao Yan Chen Zhen yu Lu 《Neural Regeneration Research》 SCIE CAS CSCD 2007年第10期611-616,共6页
At present, pathogenesis and mechanism of Parkinson disease (PD) are still unclear. Animal models of PD are essential tools in studies on etiology and therapy and should mimic the chronic pathological process, histo... At present, pathogenesis and mechanism of Parkinson disease (PD) are still unclear. Animal models of PD are essential tools in studies on etiology and therapy and should mimic the chronic pathological process, histological characteristics and motor behavior dysfunction. In recent years, transgenic mice have been widely utilized to study the mechanism of PD, and it has become imperative that a PD mouse model of motor behavioral dysfunction be established. OBJECTIVE: To compare the behavioral and histochemical characters of two neurotoxic mice model induced with 6-hydroxydopamine (6-OHDA) or 1-methyl-4-phenyl-1, 2, 3, 6 -tetrahydropyridine (MPTP), and a better method to mimic Parkinson disease will be found out. DESIGN: Parallel experiment. SETTING: Laboratory of Molecular Genetics, Department of Medical Genetics, Shanghai Jiao Tohg University. MATERIALS: Sixty 129Sv/C57BL6J male wild mice, SPF grade, 8 - 12 weeks old, weighing 20 - 25 g, were provided by Experimental Animal Center, Shanghai Jiao Tong University. All the surgery operation was performed according to the rules of Shanghai Jiaotong University Animal Committee. METHODS: The experiment was carried out in the Laboratory of Molecular Genetics (National Key Laboratory), Department of Medical Genetics, Shanghai Jiao Ttong University from March to August 2006. ①Thirty-two male mice were randomly divided into control group and drug treatment group with 16 mice in each group. Surgery was carried out and 6-OHDA was administrated to substantia nigra pars compacta (SNpc) and nigra-striatum pathway according to the different parameters with intoxication apparatus. Saline was injected to the other 16 mice according to the same paradigm. 1 mg/kg apomorphine was injected intraperitoneally 2 weeks later after surgery to induce the imbalanced rotation behavior for 40 minutes. ②Twenty-eight mice were randomly divided into 4 groups with 7 in each group, including low-dose, moderate-dose, high-dose groups and negative control group. Then, mice in the drug treatment group were injected intraperitoneally with 5, 10 and 15 mg/kg MPTP for 9 successive days. In addition, mice in the control group were injected with the same volume of saline for 9 days. Pole test and stride length test were utilized to detect coordinative behavioral dysfunction. Mice were sacrificed 20 days after MPTP treatment, and histochemical staining of tyrosine hydroxynase (TH) was used to observe the loss of dopaminergic neuron in SNpc. MAIN OUTCOME MEASURES: ① Success ratio of each model establishment method; ② inducible asymmetric cycle behavior test 2 weeks after 6-OHDA injection; ③behavioral dysfunction in pole test and stride length, morphological changes in brain tissue. RESULTS: Totally sixty mice were used in this experiment and 3 mice were excluded because of the hypersensitivity or the clumsy reaction in motor behavioral detection before MPTP treatment, therefore, data was analyzed with the rest 57 mice. ① Lethal ratio: Three out of 16 mice died in striatum injection group and 5 out of 16 mice died in nigro-striatal pathway group. No mouse died in MPTP treatment groups. ② Locomotor behavior: No dysfunction of locomotor was found in 6-OHDA treatment groups. However, several motor behavioral dysfunction were start to present at the 4th day of MPTP injection. ③ Asymmetric cycle behavior: No asymmetric cycle was induced successfully two weeks after 6-OHDA surgery. Mice show hypersensitive behavior 10 minutes after apomorphine injection, which lasted for about 20 minutes. ④ Pole test: From the 4^th day of MPTP treatment, mice started to display coordinate dysfunction, such as climbing down along the pole in spiral, moving slowly with hesitation. Some mice could not grab the pole and slide down along the pole at 4th day post injection. Comparing with 0 dose control group, all the threedrug treatment groups show significant different dysfunction from the 4th day to the 20th day post injection (P 〈 0.01). ⑤ stride length test: Mice's stride length decreased, when treated with MPTP, and the mice in the high dose group displayed obviously. ⑥ Dopaminergic neuron stained with TH in nigra pars compacta: The results indicated that administrated MPTP (from low dose to high dose) by intraperitoneal cause chronic lesions on the dopaminergic neuron in the SNpc. CONCLUSION: PD mice models induced with 6-OHDA show high mortality ratio and no asymmetric cycle was found after apomorphine injection. However, injection of MPTP intraperitoneally can simulate the chronic pathway of PD, typical histological changes are found and stable motor behavioral dysfunctions are displayed. 展开更多
关键词 Parkinson disease 6-HYDROXYDOPAMINE 1-methyl-4-phenyl-1 2 3 6-tetrahydropyridine motor behavioral dysfunction
下载PDF
Synthesis,Crystal Structure and Anti-tumor Activity of 2-(2-Chloro-4-nitrophenyl)-4-(4-chlorophenyl)-3a,4-diethoxy-2,3,3a,4-tetrahydrochromeno[3,4-d][1,2,3]diazaphosphole
16
作者 应华洲 孙茂堂 +1 位作者 刘滔 胡永洲 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2008年第10期1171-1174,共4页
The title compound 2-(2-chloro-4-nitrophenyl)-4-(4-chlorophenyl)-3a,4- diethoxy- 2,3,3a, 4-tetrahydrochromeno[3,4-d][1,2,3]diazaphosphole 2 (C29H30Cl2N3O7P, Mr = 633.44) was synthesized and its structure was cha... The title compound 2-(2-chloro-4-nitrophenyl)-4-(4-chlorophenyl)-3a,4- diethoxy- 2,3,3a, 4-tetrahydrochromeno[3,4-d][1,2,3]diazaphosphole 2 (C29H30Cl2N3O7P, Mr = 633.44) was synthesized and its structure was characterized by IR, MS, ^1H NMR, ^13C NMR, ^31p NMR, elemental analysis and single-crystal X-ray diffraction. It crystallizes in triclinic, space group P1^-, a = 9.1549(3), b = 10.7168(4), c = 17.6272(6)A, α = 102.9363(12), β = 90.2713(9), γ = 117.4265(10)°, V= 1484.41(9)A^3, Z= 2,μ(MoKa) = 0.323, F(000) = 658, Z= 2, De= 1.417 g/cm^3, the final R = 0.0687 and wR = 0.2066 for 4943 observed reflections (I 〉 2σ(I)). X-ray analysis reveals that the diazaphospholine ring is almost planar and the two ethoxy groups bonded on the 3a- and 4-positions are in trans configurations. Its antiproliferative activity was also tested in vitro against four human tumor cell lines. 展开更多
关键词 SYNTHESIS crystal structure 2-(2-chloro-4-nitrophenyl)-4-(4-chlorophenyl)-3a 4-diethoxy-2 3 3a 4-tetrahydrochromeno[3 4-d] [1 2 3]dlazaphosphole ANTITUMOR
下载PDF
THE EFFECTS OF DEPRENYL AND 1-METHYL-4-PHENYL-1, 2, 3, 6-TETRAHYDROPYRIDINE (MPTP) ON 2-DEOXYGLUCOSE UPTAKE IN THE MOUSE BRAIN
17
作者 陈生弟 徐德隆 +1 位作者 周孝达 钱可久 《Medical Bulletin of Shanghai Jiaotong University》 CAS 1992年第1期70-74,共5页
~3H-2-deoxyglucose (2-DG) autoradiographic technique was used to study the ef feets of a monoamine-oxidase-B (MAO-B) inhibitor deprenyl and the neurotoxin Ⅰ-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP) on 2-D... ~3H-2-deoxyglucose (2-DG) autoradiographic technique was used to study the ef feets of a monoamine-oxidase-B (MAO-B) inhibitor deprenyl and the neurotoxin Ⅰ-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP) on 2-DG uptake in the mouse brain. Following MPTP intoxication, 2-DG uptake was increased in the substantia nigra and lo(?)us ceruleus. At the same time, obvious abnormal behavior of the animals was induced. In the mice pretreated with deprenyl, 2-DG uptake was similar to that of control animal. Ab normal behavior. though present, was significantly milder than in mice given MPTP alone. It is concluded that MPTP interferes with the glucose metabolism in the substantia nigra and locus ceruleus and induces remarkable abnormal behavioral syndrome of mice. These deleterious effects can be blocked by pretreatment with deprenyl. 展开更多
关键词 ~3H-2-deoxyglucose autoradiography DEPRENYL 1-methyl-4-phenyl-1 2 3 6—tetrahydropyridine
下载PDF
MADOPAR-INDUCED DYSKINESIA IN 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE (MPTP) HEMIPARKINSONIAN MONKEY MODEL
18
作者 陈生弟 周孝达 +3 位作者 钱可久 徐德隆 唐琴梅 徐修蓉 《Medical Bulletin of Shanghai Jiaotong University》 CAS 1991年第1期41-46,共6页
Infusion of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) into the right common carotid artery produced hemiparkinsonian syndrome on contralateral limbs in 5 rhesus monkeys. The hemiparkinsonian syndrome produce... Infusion of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) into the right common carotid artery produced hemiparkinsonian syndrome on contralateral limbs in 5 rhesus monkeys. The hemiparkinsonian syndrome produced responded to madopar medication and the circling motion changed from toward the MPTP-treated side to away from the MPTP-treated side. Long term use of madopar developed a peak-dose dyskinesia of the face and limbs at the contralateral side. The toxic effect of MPTP was confirmed biochemically by reduction of nigrostriatal DA and histologically by degeneration of nigral neurons on the MPTP-treated side. It is concluded that this hemiparkinsonian monkey model will be of value in the elucidation of the neural mechanism underlying L-DOPA or DA agonists induced dyskinesia in Parkinson’s disease and in the search for newer methods of treatment which would produce less dyskinesia. 展开更多
关键词 DYSKINESIA MADOPAR hemiparkinsonism rhesus MONKEY 1-methyl-4-phenyl-1 2 3 6-TETRAHYDROPYRIDINE (MPTP)
下载PDF
Synthesis and Crystal Structure of S-(+)-N′-Tertbutylaminocarbonyl-N-[3-methyl-2-(4-chlorophenyl)butyryl] Thiourea
19
作者 SUN Chuan-Wen ZHANG Xiao-Dong 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2007年第2期153-156,共4页
The title compound S-(+)-N'-tertbutylaminocarbonyl-N-[3-methyl-2-(4-chlorophenyl)butyryl] thiourea has been synthesized and its crystal structure was determined by singlecrystal X-ray diffraction analysis. There... The title compound S-(+)-N'-tertbutylaminocarbonyl-N-[3-methyl-2-(4-chlorophenyl)butyryl] thiourea has been synthesized and its crystal structure was determined by singlecrystal X-ray diffraction analysis. There exist intramolecular N(2)-H(2A)…O(1), C(17)-H(17A)… O(2) and N(3)-H(3A)…S(1) hydrogen bonds as well as intermolecular N-H…O interaction between the carbonyl and amidogen groups. Crystallographic data: CITH24ClN3O2S, Mr = 369.90, monoclinic, space group C2/c with a = 22.9922(19), b = 14.4844(12), c = 12.4618(11) A, β = 92.608(2)°, V = 4145.8(6) ]k3, Z = 8, Dc = 1.185 g/cm^3, F(000) = 1568, g(MoKa) = 0.298 mm^-1, R = 0.0578 and wR = 0.1308. 展开更多
关键词 crystal structure S-(+)-3-methyl-2-(4-chlorophenyl)butyryl thiourea antiviral activity
下载PDF
Enamine Configuration of 5-Methyl-2-phenyl-4- [(Z)-3-tolylamino-phenylmethylene]pyrazol-3(2H)-one
20
作者 QIAO Yu-Qin Lü Xing-Qiang +1 位作者 BAO Feng KANG Bei-Sheng 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2005年第8期957-961,共5页
Compound 5-methyl-2-phenyl-4-[(Z)-3-tolylamino-phenylmethylene]pyrazol-3(2H)-one (C24H21N3O) crystallizes in the triclinic system, space group P1, with a = 9.267(3), b = 9.904(4),c = 12.035(4) A°, α ... Compound 5-methyl-2-phenyl-4-[(Z)-3-tolylamino-phenylmethylene]pyrazol-3(2H)-one (C24H21N3O) crystallizes in the triclinic system, space group P1, with a = 9.267(3), b = 9.904(4),c = 12.035(4) A°, α = 97.896(6), β = 103.865(6), γ = 107.950(6)°, Mr= 367.44, Z = 2, V = 993.2(6)A°^3,Dc = 1.229 g/cm^3,μ(MoKa) = 0.077 mm^-1 and F(000) = 388. The structure was refined to R =0.0444 and wR = 0.1199 for 2903 observed reflections (I 〉 2σ(I)). The results of ^1H NMR and single-crystal X-ray diffraction studies showed the enamine character of the compound. The strong intramolecular hydrogen bonds in the large conjugate system, together with weak intermolecular C-H……π hydrogen bonding and π……π stacking, lead to the formation of a multi-dimensional supramolecular network. 展开更多
关键词 5-methyl-2-phenyl-4-[(Z)-3-tolylamino-phenylmethylene]pyrazol-32H)-one enamine weak interaction snpramolecnlar network
下载PDF
上一页 1 2 3 下一页 到第
使用帮助 返回顶部