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Synthesis, Structural Characterization and Antimicrobial Activity of a Novel Cobalt(II) Complex Based on 3-Methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
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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
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Synthesis, Structural Characterization and Antimicrobial Activity of a Novel Cobalt(II) Complex Based on 3-Methyl-1-Phenyl-4-(2-Thienoyl)-Pyrazol-5-One
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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
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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
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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
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Extraction Behavior of Rare Earths with 1-phenyl-3-methyl-4-benzoyl-pyrazolone-5 Using Solid-liquid Extraction Technique 被引量:2
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作者 高锦章 潘仲巍 +2 位作者 杜新贞 康敬万 白光弼 《Rare Metals》 SCIE EI CAS CSCD 1993年第3期198-202,共5页
The extraction behavior of rare earths was studied by using paraffin with ceresin as a diluent containing 1-phenyl-3-methyl-4-benzoyl-pyrazolone-5.In solid phase,the composition of complexes is REP_3.The equilib- rium... The extraction behavior of rare earths was studied by using paraffin with ceresin as a diluent containing 1-phenyl-3-methyl-4-benzoyl-pyrazolone-5.In solid phase,the composition of complexes is REP_3.The equilib- rium extraction constants and pH_(1/2) values of solid-liquid extraction are higher than those of normal liquid-liquid extraction.The extraction efficiency tends to maximum when the ratio of phases is 1:1.When the extraction temperature is higher than the melting point of paraffin and the extraction time is over 10 min,the extraction efficiency keeps constant.Moreover,the relationship among separation factor,equilibrium extrac- tion constant,pH_(1/2) value and atomic number was obtained.The mechanism of solid-liquid extraction is analogous to that of liquid-liquid extraction. 展开更多
关键词 Solid-liquid extraction Rare earths 1-phenyl-3-methyl-4-benzoyl-pyrazolone-5
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Organic Synthesis in Ionic Liquids: Condensation of 3-Methyl-1-phenyl-5-pyrazolone with Carbonyl Compounds Catalyzed by Ethylenediammonium Diacetate (EDDA) 被引量:1
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作者 Yi HU Ping WEI +2 位作者 Hua ZHOU Ping Kai OUYANG Zhen Chu CHEN 《Chinese Chemical Letters》 SCIE CAS CSCD 2006年第3期299-301,共3页
关键词 Ionic liquids CONDENSATION 3-methyl-1-phenyl-5-pyrazolone.
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Synthesis of 1-(2-Hydroxyphenyl)-3-Phenyl-1,3-Propanedione and Luminescence Properties of Its Europium Complexes 被引量:1
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作者 Liu Shengli Qi Susu 《Journal of Rare Earths》 SCIE EI CAS CSCD 2005年第5期610-610,共1页
Using 2'-Hydroxyacetophenone and as the raw material, 1-( 2-Hydroxyphenyl )-3-Phenyl-1, 3- Propanedione (HPPPD) was synthesized by esterification reaction and Fries rearrangement reaction. And the complexes of HP... Using 2'-Hydroxyacetophenone and as the raw material, 1-( 2-Hydroxyphenyl )-3-Phenyl-1, 3- Propanedione (HPPPD) was synthesized by esterification reaction and Fries rearrangement reaction. And the complexes of HPPPD with europium were also synthesized. The compounds were characterized by IR, thermo-gravimetric analysis and ^1H-NMR. The effects of phenolic hydroxyl on the luminescence properties of complexes were studied. The results show that the complexes emit strong red fluorescence and the fluorescence intensity of the ternary complex is better than that of the duality. But the complexes of HPPPD with Sm( Ⅲ ), Tb ( Ⅲ ), Dy ( Ⅲ ) emit weak fluorescence. The phenomenon was interpreted by electron-effect and energy-matching mechanism. Energy transfer mechanism of the luminescence in the complex was discussed. 展开更多
关键词 1-(2-hydroxyphenyl)-3-phenyl-1 3-propanedione EUROPIUM COMPLEX LUMINESCENCE rare earths
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Insight into the Detailed Mechanism of HRh(CO)(PPh_3)_3 Catalyzed Hydroformylation of 1-Phenyl-1-(3-pyridyl)ethene:A DFT Study
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作者 罗小玲 梁国明 +1 位作者 李荣 孙宇阳 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第5期789-795,共7页
Density functional calculations have been used to study the mechanism of 1-phenyl-1-(3-pyridyl)ethene hydroformylation using rhodium catalyst.Our calculations reveal that the rate-determining step is the oxidative a... Density functional calculations have been used to study the mechanism of 1-phenyl-1-(3-pyridyl)ethene hydroformylation using rhodium catalyst.Our calculations reveal that the rate-determining step is the oxidative addition of hydrogen molecule and the preferred path is the one involving ts3ans for the lowest activation free-energy (ΔrGa),63.8 kJ/mol.This reaction is demonstrated to be strong exothermic by-96.6 kJ/mol of branched products and-98.2 kJ/mol of linear products.And the predominant product is the linear 3-phenyl-3-(3-pyridal)propanal (pr-ns) determined by both thermodynamics and kinetics.These results are in agreement with the practicality experimental studies. 展开更多
关键词 HYDROFORMYLATION 1-phenyl-1-(3-pyridyl)ethane Rh catalyst regioselectivity B3LYP
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Two New Schiff Bases Based on 5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde: Syntheses, Crystal Structures and Properties
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作者 孙凤梅 韩琼 +4 位作者 蒋正静 赵潘祥 王佳 芮佳怡 徐继明 《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
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Establishing motor disorder mouse models of Parkinson disease Comparison of 6-hydroxydompamine and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine
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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
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Studies on the Oxazaborolidine-catalyzed Enantioselective Reduction of 3-Morpholin-4-yl-1-phenyl-1-propanone with Density Functional Theory
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作者 FANJian-Fen LUYun-Xiang WANGQiu-Xia WULi-Fen SUNYun-Peng 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 北大核心 2005年第4期413-418,共6页
Density functional theory (DFT) has been applied to study the enantioselective reduction of 3-morpholin-4-yl-1-phenyl-1-propanone with borane catalyzed by (S)-4-benzyl-5,5- diphenyl-1,3,2-oxazaborolidine at the B3LY... Density functional theory (DFT) has been applied to study the enantioselective reduction of 3-morpholin-4-yl-1-phenyl-1-propanone with borane catalyzed by (S)-4-benzyl-5,5- diphenyl-1,3,2-oxazaborolidine at the B3LYP/6-31G* level. All molecular species involved in the four reaction steps have been fully optimized and the structural parameters are provided, and the micro process of reaction was also investigated. The catalyst-alkoxyborane adduct formed in step III exhibits a B-O-B-N tetra-atomic ring. Reaction coordination calculations show that BH3 can react with 3-morpholin-4-yl-1-phenyl-1-propanone spontaneously, resulting in the need of 2 mol BH3 in the reaction. 展开更多
关键词 B3LYP/6-31G* 3-morpholin-4-yl-1-phenyl-1-propanone enantioselective reduction
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THE EFFECTS OF DEPRENYL AND 1-METHYL-4-PHENYL-1, 2, 3, 6-TETRAHYDROPYRIDINE (MPTP) ON 2-DEOXYGLUCOSE UPTAKE IN THE MOUSE BRAIN
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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
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MADOPAR-INDUCED DYSKINESIA IN 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE (MPTP) HEMIPARKINSONIAN MONKEY MODEL
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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)
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Synthesis and Crystal Structure of Methyl 2-(Diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate
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作者 Ali Souldozi Seyed Hamid Reza Shojaei +2 位作者 Ali Ramazani Katarzyna lepokura Tadeusz Lis 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2013年第1期82-88,共7页
The title compound, methyl 2-(diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate, was synthesized and studied by single-crystal X-ray diffraction method. The structure of the product was confirmed by IR, 1H- and 13C... The title compound, methyl 2-(diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate, was synthesized and studied by single-crystal X-ray diffraction method. The structure of the product was confirmed by IR, 1H- and 13C-NMR spectroscopy and elemental analysis. These experimental studies were supported by quantum mechanical calculations. The structure was solved in monoclinic, space group P21/c with a = 9.573(3), b = 19.533(7), c = 9.876(3), β = 92.35(4)°, V = 1845.2(10)3, T = 85(2) K, Z = 4, R = 0.040 and wR = 0.089 for 6424 observed reflections with I2σ(I). 展开更多
关键词 single-crystal X-ray structure multi-component reaction methyl 2-(diphenylamino)-4-phenyl-1 3-thiazole-5-carboxylate benzoyl isothiocyanate DIPHENYLAMINE dimethyl acetylenedicarboxylate
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Prenatal and Postnatal Exposures to 1-Methyl-4-phenyl-1,2,3,6-tetra Hydropyridine (MPTP) Impaired Mouse Midbrain Dopamine System and May Produce a Predisposing and Inducing Model for Parkinson’s Disease
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作者 Gladson Muthian Jennifer King +3 位作者 Lemuel Dent Marquitta Smith Veronica Mackey Clivel Charlton 《Journal of Behavioral and Brain Science》 2012年第4期485-494,共10页
Dopamine cell bodies in the substantia nigra of the midbrain and with their terminals projecting to the neostriatum form the nigrostriatum and these dopamine neurons degenerate in Parkinson’s disease (PD). Based on m... Dopamine cell bodies in the substantia nigra of the midbrain and with their terminals projecting to the neostriatum form the nigrostriatum and these dopamine neurons degenerate in Parkinson’s disease (PD). Based on metabolic and func- tional specialization of the cell bodies versus the axon terminals, the level and disposition of dopamine, its metabolites and enzymes are different in both regions and are likely to be affected differently in PD. We examined changes in the midbrain dopamine system following 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), to test the hypothesis that a predisposing/sensitization stage and a inducing/precipitating stage underlie PD. Pregnant mice were treated with a low dose of MPTP during gestation days 8 - 12 to model the predisposing/sensitization stage, by interrupting the fetal mid- brain dopamine system during its neurogenesis. For the inducing/precipitating stage, the 12-weeks offspring were ad- ministered MPTP. The prenatal-MPTP offspring appear normal, but midbrain dopamine, 3,4-di-hydroxy-phenyl-acetic- acid, 3-methoxytyramine, tyrosine-hydroxylase and L-aromatic-amino-acid-decarboxylase, were reduced by 49.6%, 48%, 54%, 20.9% and 25%. Postnatal-MPTP of 10, 20, 30 mg/kg administered to the prenatal-PBS vs prenatal-MPTP offspring reduced midbrain dopamine by 43.6%, 47.2%, 70.3% vs 85.4%, 89.1%, 95.2%;tyrosine-hydroxylase by 30%, 63%, 81% vs 30.7%, 70.4%, 91.4%;L-aromatic-amino-acid-decarboxylase by 0%, 2%, 40% vs 32%, 40%, 58%. The prenatal-MPTP may render the DA system sensitive by causing sub-threshold reduction of DA, its metabolites and en- zymes, enabling postnatal-MPTP to reduce dopamine above the 70% - 80% PD-inducing threshold. Thus, the study may produce a prenatal predisposing/sensitization and postnatal inducing/precipitation model of PD. It also indicates that some cases of PD may have a fetal basis, in which sub-threshold nigrostriatal impairments occur early in life and PD-symptoms are induced during aging by further insults to the dopaminergic system that would not cause PD symptoms in normal indi-viduals. 展开更多
关键词 Parkinson’s Disease MIDBRAIN 1-Methyl-4-phenyl-1 2 3 6-TETRAHYDROPYRIDINE (MPTP) Dopamine Tyrosine Hydroxylase L-aromatic Amino Acid Decarboxylase Sensitization Precipitation
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Aspects on the Mechanism of the 1-Phenyl-1<i>H</i>-pyrazolo[3,4-<i>b</i>]quinoxaline Formation
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作者 Mohamed A. Mostafa Salah L. Aboulela +2 位作者 Mohammed A. E. Sallam Farida F. Louis Thorleif Anthonsen 《Green and Sustainable Chemistry》 2012年第2期71-75,共5页
Condensation of D-glucose, o-phenylenediamine and N,N-benzylphenylhydrazine hydrochloride (NNBPHH) in a one-pot reaction, or condensation of 2-(D-arabino-tetritol-1-yl) quinoxaline and NNBPHH, gave 3-(D-erythro-glycer... Condensation of D-glucose, o-phenylenediamine and N,N-benzylphenylhydrazine hydrochloride (NNBPHH) in a one-pot reaction, or condensation of 2-(D-arabino-tetritol-1-yl) quinoxaline and NNBPHH, gave 3-(D-erythro-glycerol-1- yl)-1-phenyl-1H-pyrazolo[3,4-b]quinoxaline. The structure of the latter was determined by 1H NMR spectroscopy and by synthesis using phenylhydrazine hydrochloride instead of NNBPHH. Condensation of D-glucose and 4,5-dichloro-o-phenylenediamine gave 6,7-dichloro-2-(D-arabino-tetritol-1-yl)quinoxaline, which upon condensation with NNBPHH gave the corresponding 6,7-dichloro-3-(D-erythro-glycerol-1-yl)-1-phenyl-1H-pyrazolo[3,4-b]quinoxaline. The structure and mechanism of formation of these compounds are discussed. 展开更多
关键词 2-(D-arabino-tetritol-1-yl)quinoxaline Pyrazolo[3 4-b]quinoxalines 3-(D-erythro-glycerol-1-yl)-1-phenyl-1H-pyrazolo-[3 4-b]qunoxaline 4 5-Dichloro-o-phenylenediamine 6 7-Dichloro-2-(D-arabino-tetritol-1-yl)quinoxaline 7-Dichloro-3-(D-erythro-glycerol-1-yl)-1-phenyl-1H-pyrazolo-[3 4-b]quinoxaline N N-Benzylphenylhydrazine hydrochloride
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1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉的合成与生物活性 被引量:1
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作者 江银枝 石雅义 +2 位作者 邹洋 梁大伟 周俊 《浙江理工大学学报(自然科学版)》 2012年第5期730-733,共4页
研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplate... 研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplater和FieldAlign计算化合物和已知的EcMetAP酶抑制剂的空间作用力场的相似性。共合成了6个1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉类化合物,但只有化合物5对EcMetAP酶活性有抑制作用,抑制率为31.62%,空间作用力场的相似度为0.615。说明化合物5可作为先导化合物进行结构优化,得到优良的EcMetAP酶抑制活性化合物。 展开更多
关键词 吡唑啉 合成 大肠杆菌甲硫酰胺肽酶 构效关系1-phenyl-3-(2-Hydroxyl—Phenyl)-5-Diaryl-2-
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Solid State Synthesis and Crystal Structure of 3—Methly—1—phenyl—4—phe
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作者 杜大明 祝英 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 1995年第4期277-280,共4页
The solid state thermal reaction of benzil with 3-methyl-1-phenyl-5-pyrazolone gave the title compound 1 (C_24H_18N_2O_2) and its isomer 2. The crystal structure of the title compound has been determined by X-ray anal... The solid state thermal reaction of benzil with 3-methyl-1-phenyl-5-pyrazolone gave the title compound 1 (C_24H_18N_2O_2) and its isomer 2. The crystal structure of the title compound has been determined by X-ray analysis. The crystal belongs to monoclinic system, space group P2_1/n, with cell parameters a = 7. 479 ( 1 ), b =16. 992(1), c=15. 165(1) A , β= 100. 99(1)°, V= 1891. 9 A ̄3, M_r=366. 42, Z=4, D_c= 1. 286 g/cm ̄3, μ= 6. 236 cm ̄-1, F(000) = 768. In the molecule of 1, benzoyl group and CO group of five-member ring are in cis-positions, the interaction of oxygen atoms leads to the noncoplanarity. 展开更多
关键词 solid state reaction BENZIL 3-methyl-1-phenyl-5-pyrazolone crystal structure
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Exendin-4 and linagliptin attenuate neuroinflammation in a mouse model of Parkinson's disease 被引量:6
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作者 Hai-Yang Yu Tong Sun +7 位作者 Zhen Wang Hong Li Duo Xu Jing An Lu-Lu Wen Jia-Yi Li Wen Li Juan Feng 《Neural Regeneration Research》 SCIE CAS CSCD 2023年第8期1818-1826,共9页
Use of glucagon-like peptide-1 receptor agonist or dipeptidyl peptidase 4 inhibitor has been shown to lower the incidence of Parkinson's disease in patients with diabetes mellitus.Therefore,using these two treatme... Use of glucagon-like peptide-1 receptor agonist or dipeptidyl peptidase 4 inhibitor has been shown to lower the incidence of Parkinson's disease in patients with diabetes mellitus.Therefore,using these two treatments may help treat Parkinson's disease.To further investigate the mechanisms of action of these two compounds,we established a model of Parkinson's disease by treating mice with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and then subcutaneously injected them with the glucagon-like peptide-1 receptor agonist exendin-4 or the dipeptidyl peptidase 4 inhibitor linagliptin.We found that both exendin-4 and linagliptin reversed motor dysfunction,glial activation,and dopaminergic neuronal death in this model.In addition,both exendin-4 and linagliptin induced microglial polarization to the anti-inflammatory M2 phenotype and reduced pro-inflammatory cytokine secretion.Moreover,in vitro experiments showed that treatment with exendin-4 and linagliptin inhibited activation of the nucleotide-binding oligomerization domain-and leucine-rich-repeat-and pyrin-domaincontaining 3/caspase-1/interleukin-1βpathway and subsequent pyroptosis by decreasing the production of reactive oxygen species.These findings suggest that exendin-4 and linagliptin exert neuroprotective effects by attenuating neuroinflammation through regulation of microglial polarization and the nucleotidebinding oligomerization domain-and leucine-rich-repeat-and pyrin-domain-containing 3/caspase-1/interleukin-1βpathway in a mouse model of Parkinson's disease induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine.Therefore,these two drugs may serve as novel anti-inflammatory treatments for Parkinson's disease. 展开更多
关键词 diabetes mellitus dipeptidyl peptidase 4 inhibitor EXENDIN-4 glucagon-like peptide-1 receptor agonist 1-methyl-4-phenyl-1 2 3 6-TETRAHYDROPYRIDINE LINAGLIPTIN microglia NEUROINFLAMMATION NLRP3 inflammasome Parkinson's disease PYROPTOSIS
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The transient receptor potential melastatin 2:a new therapeutical target for Parkinson's disease? 被引量:2
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作者 Ana Flávia F.Ferreira Luiz Roberto G.Britto 《Neural Regeneration Research》 SCIE CAS CSCD 2023年第8期1652-1656,共5页
The transient receptor potential melastatin 2 is a calcium-permeable cation channel member of the TRP family. Also known as an oxidative stress-activated channel, the transient receptor potential melastatin 2 gating m... The transient receptor potential melastatin 2 is a calcium-permeable cation channel member of the TRP family. Also known as an oxidative stress-activated channel, the transient receptor potential melastatin 2 gating mechanism is dependent on reactive oxygen species. In pathological conditions, transient receptor potential melastatin 2 is overactivated, leading to a Ca~(2+) influx that alters cell homeostasis and promotes cell death. The role of transient receptor potential melastatin 2 in neurodegenerative diseases, including Alzheimer's disease and ischemia, has already been described and reviewed. However, data on transient receptor potential melastatin 2 involvement in Parkinson's disease pathology has emerged only in recent years and the issue lacks review studies that focus specifically on this topic. The present review aims to elucidate the role of the transient receptor potential melastatin 2 channel in Parkinson's disease by reviewing, summarizing, and discussing the in vitro, in vivo, and human studies published until August 2022. Here we describe fourteen studies that evaluated the transient receptor potential melastatin 2 channel in Parkinson's disease. The Parkinson's disease model used, transient receptor potential melastatin 2 antagonist and genetic approaches, and the main outcomes reported were discussed. The studies described transient receptor potential melastatin 2 activation and enhanced expression in different Parkinson's disease models. They also evidenced protective and restorative effects when using transient receptor potential melastatin 2 antagonists, knockout, or silencing. This review provides a literature overview and suggests where there is a need for more research. As a perspective point, this review shows evidence that supports transient receptor potential melastatin 2 as a pharmacological target for Parkinson's disease in the future. 展开更多
关键词 1-methyl-4-phenyl-1 2 3 6-tetrahydropyridine(MPTP) 1-methyl-4-phenylpyridinium(MPP+) 6-HYDROXYDOPAMINE AG490 CLOTRIMAZOLE flufenamic acid N-(p-amylcinnamoyl)anthranilic acid Parkinson's disease poly-ADPR polymerase type 1(PARP1) ROTENONE PARAQUAT transient receptor potential melastatin 2(TRPM2)
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Syntheses and Crystal Structure of Six-coordinated Diorgnotin Complexes with 2,5-Dimercapto-4-phenyl-1,3,4-thiodiazole
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作者 马春林 马春林 +2 位作者 李凤 张如芬 王大奇 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2003年第7期847-852,共6页
The reactions of diorganotin dichloride [Ph2SnCl2, (PhCH2)2-SnCl2 or (n-Bu)2SnCl2] with potassium salt of 2,5-dimercapto-4-phenyl-1, 3,4-thiodiazole gave complexes R2Sn (S3N2C8H5)2 (4: R = Ph; 5: R = PhCH2 and 6: R = ... The reactions of diorganotin dichloride [Ph2SnCl2, (PhCH2)2-SnCl2 or (n-Bu)2SnCl2] with potassium salt of 2,5-dimercapto-4-phenyl-1, 3,4-thiodiazole gave complexes R2Sn (S3N2C8H5)2 (4: R = Ph; 5: R = PhCH2 and 6: R = n-Bu), respectively. Characterizations were carried out for all complexes by IR, 'H NMR spectra and X-ray crystallography analysis. Including the Sn…N interaction, the three complexes all have six-coordinated distorted octahedral geometry. Based on the requence of stereo-chemical constraint sequence, phenyl≈benzyl > n-butyl, the less the effect of the stereochemical constraint of R groups, the shorter the Sn…N length. In complexes 5 and 6, there exist S…S weak intra-molecular interactions, through which the complexes are dissociated into loose 2D polymers. All three complexes show antitumour activity in bioactivity measurements. 展开更多
关键词 2 5-dimercapto-4-phenyl-1 3 4-thiodiazole X-ray crystallography DIORGANOTIN CHELATE
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