~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
The chemical reactivity of novel stable triazene 3 toward some nucleophilic and electrophilic reagents was investigated. Traizene 3 was used as a key precursor for the synthesis of some novel important heterocyclic co...The chemical reactivity of novel stable triazene 3 toward some nucleophilic and electrophilic reagents was investigated. Traizene 3 was used as a key precursor for the synthesis of some novel important heterocyclic compounds such as Pyrazole, Isoxazole, Dihydropyrimidine, Tetrahydro-pyridine derivatives with expected antimicrobial activity. The synthesized compounds were obtained in good yields. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H-NMR and Ms spectral data.展开更多
Phosphine-catalyzed [4+2] annulations of 2-(acetoxymethyl)buta-2,3-dienoates with α-aminonitriles have been developed, in which a-aminonitriles serve as C, N-bisnucleophilic reaction partners and 2-(acetoxymethyl...Phosphine-catalyzed [4+2] annulations of 2-(acetoxymethyl)buta-2,3-dienoates with α-aminonitriles have been developed, in which a-aminonitriles serve as C, N-bisnucleophilic reaction partners and 2-(acetoxymethyl)buta- 2,3-dienoates as "C4 synthons" respectively. A number of a-aminonitriles could be successfully applied to giving multifunctional desired products using PPh3 as catalyst. This method provides a facile entry to access polysubstituted tetrahydropyridines bearing quaternary carbon centers. The possible reaction mechanism was also proposed.展开更多
The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C5...The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C57BL/6J mice treated with 1-methyl-4-phenyl-1,2, 3, 6-tetrahydropyridine (MPTP) Bax protein expression was significantly reduced in isatin (100, 200 mg/kg)-pretreated mice. Results demonstrate that isatin plays a neuroprotective role in mice treated with MPTP by down-regulating Bax protein expression.展开更多
5-(5"-Substituted phenyl-[1",3",4"]oxadiazol-2"-yl methylsulfanyl)-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a...5-(5"-Substituted phenyl-[1",3",4"]oxadiazol-2"-yl methylsulfanyl)-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a-j. The reduction of compounds 2 with NaBH4 in methanol gave the target compounds 5-(5"-substituted phenyl-[1",3",4"]oxadiazol-2"-yl methylsulfanyl)-3-(1′-methyl-1',2',5',6'-tetrahydropyridin-3'-yl)-[1,2,4]triazol-4-ylamines 3a-j. The endothelium vascular relaxing activity of the target compounds were screened.展开更多
Amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol 1 were condensed with 2-bromo-1- (substituted phenyl)ethanone to give pyridinyltriazolothiadiazines 2a^c, which were quaternarized with methyl iodide and oxidized wit...Amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol 1 were condensed with 2-bromo-1- (substituted phenyl)ethanone to give pyridinyltriazolothiadiazines 2a^c, which were quaternarized with methyl iodide and oxidized with 30 % hydrogen peroxide to afford the corresponding methyl pyridinium salts 3a^c and pyridine-1-oxides 4a^c, respectively. The reduction of compounds 3 and 4 with NaBH4 in methanol produced the target compounds 1-methyl-1, 2, 5, 6-tetrahydropyridin-3- yl)-6-aryl-s-triazolothiadiazines 5a^c and 3-(1-hydroxyl-1, 2, 5, 6-tetrahydropyridin -3-yl)-6-aryl- s-triazolothiadiazines 6a^c, respectively. The endothelium vascular relaxing activity of the target compounds was screened.展开更多
A series of 2- and 5-(1,1-dimethyl-1,2,5,6-tetrahydropyridinium-3-yl)oxadiazoline iodides, which might be used as M 1 muscarinic receptor agonists, was synthesized from nicotin-aldehyde and nicotinhydrazine, respecti...A series of 2- and 5-(1,1-dimethyl-1,2,5,6-tetrahydropyridinium-3-yl)oxadiazoline iodides, which might be used as M 1 muscarinic receptor agonists, was synthesized from nicotin-aldehyde and nicotinhydrazine, respectively. Their structures were characterized by 1H NMR, IR, MS spectra and elemental analysis.展开更多
文摘~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.
文摘The chemical reactivity of novel stable triazene 3 toward some nucleophilic and electrophilic reagents was investigated. Traizene 3 was used as a key precursor for the synthesis of some novel important heterocyclic compounds such as Pyrazole, Isoxazole, Dihydropyrimidine, Tetrahydro-pyridine derivatives with expected antimicrobial activity. The synthesized compounds were obtained in good yields. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H-NMR and Ms spectral data.
基金Supported by the National Natural Science Foundation of China(No. 21372096).
文摘Phosphine-catalyzed [4+2] annulations of 2-(acetoxymethyl)buta-2,3-dienoates with α-aminonitriles have been developed, in which a-aminonitriles serve as C, N-bisnucleophilic reaction partners and 2-(acetoxymethyl)buta- 2,3-dienoates as "C4 synthons" respectively. A number of a-aminonitriles could be successfully applied to giving multifunctional desired products using PPh3 as catalyst. This method provides a facile entry to access polysubstituted tetrahydropyridines bearing quaternary carbon centers. The possible reaction mechanism was also proposed.
基金a grant from Shandong Provincial Education Department, No. J08LH54
文摘The present study observed the action of 1H-indole-2, 3-dione (isatin) on Bax protein expression in the substantia nigra of a Parkinson's disease animal model. Parkinson's disease-like behaviors were induced in C57BL/6J mice treated with 1-methyl-4-phenyl-1,2, 3, 6-tetrahydropyridine (MPTP) Bax protein expression was significantly reduced in isatin (100, 200 mg/kg)-pretreated mice. Results demonstrate that isatin plays a neuroprotective role in mice treated with MPTP by down-regulating Bax protein expression.
基金supported by the State Basic Research and Development Project(No.G 1998051112)the Science Foundation of Henan University(04ZDZR009).
文摘5-(5"-Substituted phenyl-[1",3",4"]oxadiazol-2"-yl methylsulfanyl)-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a-j. The reduction of compounds 2 with NaBH4 in methanol gave the target compounds 5-(5"-substituted phenyl-[1",3",4"]oxadiazol-2"-yl methylsulfanyl)-3-(1′-methyl-1',2',5',6'-tetrahydropyridin-3'-yl)-[1,2,4]triazol-4-ylamines 3a-j. The endothelium vascular relaxing activity of the target compounds were screened.
基金supported by the State Basic Research and Development Project(No.G1998051112)the Science Foundation of Henan University(XK02041)
文摘Amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol 1 were condensed with 2-bromo-1- (substituted phenyl)ethanone to give pyridinyltriazolothiadiazines 2a^c, which were quaternarized with methyl iodide and oxidized with 30 % hydrogen peroxide to afford the corresponding methyl pyridinium salts 3a^c and pyridine-1-oxides 4a^c, respectively. The reduction of compounds 3 and 4 with NaBH4 in methanol produced the target compounds 1-methyl-1, 2, 5, 6-tetrahydropyridin-3- yl)-6-aryl-s-triazolothiadiazines 5a^c and 3-(1-hydroxyl-1, 2, 5, 6-tetrahydropyridin -3-yl)-6-aryl- s-triazolothiadiazines 6a^c, respectively. The endothelium vascular relaxing activity of the target compounds was screened.
文摘A series of 2- and 5-(1,1-dimethyl-1,2,5,6-tetrahydropyridinium-3-yl)oxadiazoline iodides, which might be used as M 1 muscarinic receptor agonists, was synthesized from nicotin-aldehyde and nicotinhydrazine, respectively. Their structures were characterized by 1H NMR, IR, MS spectra and elemental analysis.