A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were ...A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ ( 3-methoxyphenylsulfinyl ) methyl ] -1-methyl-4- [ (4-methylpiperazin-1-yl) methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.展开更多
The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized...The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.展开更多
One novel nickel coordination polymer, {[Ni(OTP)(bib)1.5(H2O)]·2H2O}n(1, H2 OTP = 2-hydroxy-5-(3',5'-terephthalic acid) pyridine, bib = 1,4-bis(1-imdazoly)benzene), has been synthesized and characte...One novel nickel coordination polymer, {[Ni(OTP)(bib)1.5(H2O)]·2H2O}n(1, H2 OTP = 2-hydroxy-5-(3',5'-terephthalic acid) pyridine, bib = 1,4-bis(1-imdazoly)benzene), has been synthesized and characterized by elemental analysis(EA), IR, powder X-ray diffraction(PXRD), and thermogravimetric(TG) analyses. The crystal of 1 crystallizes in monoclinic, space group P21/n with a = 12.2860(5), b = 13.8246(6), c = 19.0140(8) A, β = 104.3870(1)°, V = 3128.2(2) A3, Z = 4, C32H28N7 Ni O8, Mr = 697.32, Dc = 1.481 g/cm^3, F(000) = 1444 and μ(Mo Kα) = 0.684 mm-1. The final R = 0.0704 and w R = 0.1764 for 5485 observed reflections with I 2σ(I) and R = 0.1087 and wR = 0.2010 for all data. Topology analysis reveals that complex 1 is a 3D 2-fold interpenetrated {4^4·6^6}-nov net based on the 1D [Ni(OTP)]n chain and the 2D [Ni2(bib)3]n sql sheet. And the variable-temperature magnetic susceptibility measurements exhibit weak antiferromagnetic coupling interaction.展开更多
The title compound, 4-(tert-butyl)-5-(1 H- 1,2,4-triazol- 1 -yl)-N-(2-hydroxy-3,5-diio- dinebenzyl)thiazol-2-amine, was synthesized via the reduction of 4-(tert-butyl)-5-(1H-l,2,4- triazol-l-yl)-N-benzyliden...The title compound, 4-(tert-butyl)-5-(1 H- 1,2,4-triazol- 1 -yl)-N-(2-hydroxy-3,5-diio- dinebenzyl)thiazol-2-amine, was synthesized via the reduction of 4-(tert-butyl)-5-(1H-l,2,4- triazol-l-yl)-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944(19), b = 10.5250(3), c = 24.4985(6) A, Z = 4, V = 2041.66(9) A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F(000) = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections (I 〉 2σ(I)). X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O(2)-H(2A)…O(1), O(2)-H(2B)…N(I) and N(5)-H(5)…O(2), and an octatomic ring R^(8) is formed via intramolecular hydrogen bond of O(I)-H(IA)…N(4). Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.展开更多
A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) acti...A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine(IC50=54.78μmol/L).展开更多
Two N-donor ligands mediated Cd(Ⅱ) coordination polymers, namely,[Cd(L)(dmpz)2]n (1) and {[Cd(L)(atr)05(H20)](H2O)}n (2) (H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethy...Two N-donor ligands mediated Cd(Ⅱ) coordination polymers, namely,[Cd(L)(dmpz)2]n (1) and {[Cd(L)(atr)05(H20)](H2O)}n (2) (H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethylpyrazole, and atr= 4-amino-l,2,4-triazole), havebeen produced. Their structures were characterized by single-crystal X-ray diffraction analysis,elemental analyses and infrared spectra. Compound 1 possesses a one-dimensional (1D) chainstructure and is finally extended into a three-dimensional (3D) supramolecular architecturethough hydrogen bonding interactions. Compound 2 features a two-dimensional (2D) networkwith 4-connected sql topology based on dinuclear Cd(Ⅱ) clusters as nodes, which is alsoassembled into a 3D supramolecular architecture through hydrogen bonding interactions.Furthermore, compounds 1 and 2 exhibit high thermal stabilities and intense fluorescent emissionin the solid, and can be explored as potential luminescent materials.展开更多
A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots o...A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.展开更多
A novel method for the determination of cationic surfactant by laser thermal lens spectrometry was developed. It was based on the reaction between 1-hydroxy-2-(5-nitro-2-Pyri- dylazo)-8-aminonaphthalene-3,6-disulfoni...A novel method for the determination of cationic surfactant by laser thermal lens spectrometry was developed. It was based on the reaction between 1-hydroxy-2-(5-nitro-2-Pyri- dylazo)-8-aminonaphthalene-3,6-disulfonic acid (5-NO2-PAH) and cationic surfactant to form 1:2 ionic association complex in a weakly basic medium (pH 9.44). The determination conditions and the mechanism were discussed. The method has been applied to the analysis of wastewater and moat water samples.展开更多
A novel phenolic glucoside was isolated from stem barks of Alangium plantanifolium, its structure was elucidated to be 1-O-[2-(1-hydroxy-6-oxocyclohex-2-ene-1-carboxymethyl) -phenyl]-4, 6-O-[(S)-4, 4', 5, 5', ...A novel phenolic glucoside was isolated from stem barks of Alangium plantanifolium, its structure was elucidated to be 1-O-[2-(1-hydroxy-6-oxocyclohex-2-ene-1-carboxymethyl) -phenyl]-4, 6-O-[(S)-4, 4', 5, 5', 6, 6'-hexahydroxydi-phenoyl]-beta -D-glucopyranose 1 by spectroscopic methods including 2D NMR techniques.展开更多
This brief review discusses the behavioral consequences of two pharmacologically selected lines of rats. Flinders Sensitive (FSL) and Flinders Resistant (FRL) Lines of rats were selected on the basis of differential h...This brief review discusses the behavioral consequences of two pharmacologically selected lines of rats. Flinders Sensitive (FSL) and Flinders Resistant (FRL) Lines of rats were selected on the basis of differential hypothermic and behavioral responses to the anticholinesterase, diisopropylfluorophosphate (DFP). FSL rats are more sensitive to the hypothermic effects of cholinergic, serotonergic, and dopaminergic agonists but less sensitive to the locomotor or stereotypic effects of dopamine agonists. FSL rats exhibit greater immobility in the forced swim test and reduced social interaction compared with FRL rats, but do not differ in saccharin intake, behavior in the elevated plus maze, or responses for rewarding brain self-stimulation. The exaggerated immobility and reduced social interaction are counteracted by chronic treatment with antidepressants. Because FSL rats were more sensitive to 5-HT1A receptor agonists, high (HDS) and low (LDS) 8-OH-DPATsensitive lines were selectively bred for differential hypothermic responses to the 5-HT1A receptor agonist, 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT). HDS rats were also more sensitive to the hypothermic effects of oxotremorine, a cholinergic agonist, but selection for this response did not diverge with later selection. HDS rats exhibited greater immobility in the forced swim test than LDS rats and this correlated response could be seen early in selection (generation 3). HDS rats also showed reduced social interaction compared to LDS rats, but did not differ in behavior in the elevated plus maze. These findings confirm that selection for hypothermic responses to pharmacological agents do have behavioral consequences, notably the production of depressive-like phenotypes, which can be counteracted by chronic antidepressant treatment. Because increased 5-HT1A receptor sensitivity was common to both selected lines (FSL and HDS), neurobiological processes dependent on this receptor could contribute to the abnormal behaviors that manifest in these rat lines and thus suggesting a mechanism underlying depressive behaviors in humans. However, available human data are inconsistent with this hypothesis and suggest that other mechanisms underlie these behavioral abnormalities in HDS and FSL rats. These mechanisms as well as additional behavioral testing in these rat lines will be discussed.展开更多
Two pairs of unusual scalemic enantiomers with a dimethoxyphenyl)ethyl]-2-methoxyindolin-3-one, novel carbon skeleton of 2-[1′-(4"-hydroxy-3",5"- named isatidifoliumindolinones A-D (1-4), were isolated from an...Two pairs of unusual scalemic enantiomers with a dimethoxyphenyl)ethyl]-2-methoxyindolin-3-one, novel carbon skeleton of 2-[1′-(4"-hydroxy-3",5"- named isatidifoliumindolinones A-D (1-4), were isolated from an aqueous extract of lsatis indigotica leaves (da qing ye). Their structures including absolute configurations were determined by spectroscopic data analysis combined with comparison of their experimental CD and calculated ECD spectra. Validity of the ECD spectra calculation to assign the absolute configurations is discussed. Plausible biosynthetic pathways of 1-4 are proposed. Stereochemistry-dependent activity against LPS-induced NO production in BY2 cells was observed, and among the stereoisomers compound 4 is most active.展开更多
Two new isoflavonoid glucosides, 5-hydroxy-6,7-methylenedioxy-isoflavone-4'-O-D-glucopyranosyl (2→〉l)-L-rhamnoside (irilone-bioside) (compound 1) and 5,4'-methoxy-6,7-methylenedioxyisoflavone-3'-O-β-D-gluc...Two new isoflavonoid glucosides, 5-hydroxy-6,7-methylenedioxy-isoflavone-4'-O-D-glucopyranosyl (2→〉l)-L-rhamnoside (irilone-bioside) (compound 1) and 5,4'-methoxy-6,7-methylenedioxyisoflavone-3'-O-β-D-glucoside (irisleptophyllidin) (compound 2), together with five known compounds, nigricanin- 4'-O-β-D-glucoside (compound 3), irifloside (compound 4), irigenin (compound 5), 5, 3', 4'-trimethoxy-6,7-methylenedioxyisoflavone (compound 6), and nigricanin (compound 7) were isolated from the alcoholic extract of rhizomes of Iris leptophylla Lingelsh. Their structures were elucidated by spectroscopic methods.展开更多
基金Supported by the National Natural Science Foundation of China(No.20042047).
文摘A series of ethyl 5-hydroxyindole-3-earboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, ^1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2.2.15 cells. Among them, compound 7g { ethyl 5-hydroxy-2- [ ( 3-methoxyphenylsulfinyl ) methyl ] -1-methyl-4- [ (4-methylpiperazin-1-yl) methyl ]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.
文摘The two diarylheptanoids (E)-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl) hept-4-en-3-one 1 (Gingerenone C) and (±)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4- hydroxyphenyl)-3-heptanone 2 were synthesized from vanillin 3 and 4-hydroxybenzaldehyde 9.
基金supported by the Natural Science Foundation of Shandong Province(ZR2011BL020,ZR2012CM019)National Natural Science Foundation of China(21451001)Key Discipline and Innovation Team of Qilu Normal University
文摘One novel nickel coordination polymer, {[Ni(OTP)(bib)1.5(H2O)]·2H2O}n(1, H2 OTP = 2-hydroxy-5-(3',5'-terephthalic acid) pyridine, bib = 1,4-bis(1-imdazoly)benzene), has been synthesized and characterized by elemental analysis(EA), IR, powder X-ray diffraction(PXRD), and thermogravimetric(TG) analyses. The crystal of 1 crystallizes in monoclinic, space group P21/n with a = 12.2860(5), b = 13.8246(6), c = 19.0140(8) A, β = 104.3870(1)°, V = 3128.2(2) A3, Z = 4, C32H28N7 Ni O8, Mr = 697.32, Dc = 1.481 g/cm^3, F(000) = 1444 and μ(Mo Kα) = 0.684 mm-1. The final R = 0.0704 and w R = 0.1764 for 5485 observed reflections with I 2σ(I) and R = 0.1087 and wR = 0.2010 for all data. Topology analysis reveals that complex 1 is a 3D 2-fold interpenetrated {4^4·6^6}-nov net based on the 1D [Ni(OTP)]n chain and the 2D [Ni2(bib)3]n sql sheet. And the variable-temperature magnetic susceptibility measurements exhibit weak antiferromagnetic coupling interaction.
基金supported by the National Undergraduate Training Programs for Innovation and Entrepreneurship of Hunan Universitythe Natural Science Foundation of Hunan Province(No.12jj3012)
文摘The title compound, 4-(tert-butyl)-5-(1 H- 1,2,4-triazol- 1 -yl)-N-(2-hydroxy-3,5-diio- dinebenzyl)thiazol-2-amine, was synthesized via the reduction of 4-(tert-butyl)-5-(1H-l,2,4- triazol-l-yl)-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944(19), b = 10.5250(3), c = 24.4985(6) A, Z = 4, V = 2041.66(9) A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F(000) = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections (I 〉 2σ(I)). X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O(2)-H(2A)…O(1), O(2)-H(2B)…N(I) and N(5)-H(5)…O(2), and an octatomic ring R^(8) is formed via intramolecular hydrogen bond of O(I)-H(IA)…N(4). Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line.
基金Supported by the National Natural Science Foundation of China(No.30672519)
文摘A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-lH-indole-3-carboxylates 8a--8j and 11e--11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) activity and cytotoxicity. Among them, six compounds showed more potent inhibitory activity than lamivudine. Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L, which was 33-times more potent than the reference drug lamivudine(IC50=54.78μmol/L).
基金supported by the National Natural Science of Foundation of China(No.21671094)
文摘Two N-donor ligands mediated Cd(Ⅱ) coordination polymers, namely,[Cd(L)(dmpz)2]n (1) and {[Cd(L)(atr)05(H20)](H2O)}n (2) (H2L = methyl-3-hydroxy-5-carboxy-2-thiophenecarboxylate, dmpz = 3,5-dimethylpyrazole, and atr= 4-amino-l,2,4-triazole), havebeen produced. Their structures were characterized by single-crystal X-ray diffraction analysis,elemental analyses and infrared spectra. Compound 1 possesses a one-dimensional (1D) chainstructure and is finally extended into a three-dimensional (3D) supramolecular architecturethough hydrogen bonding interactions. Compound 2 features a two-dimensional (2D) networkwith 4-connected sql topology based on dinuclear Cd(Ⅱ) clusters as nodes, which is alsoassembled into a 3D supramolecular architecture through hydrogen bonding interactions.Furthermore, compounds 1 and 2 exhibit high thermal stabilities and intense fluorescent emissionin the solid, and can be explored as potential luminescent materials.
文摘A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.
基金supported by national 863 project(Grant No.2004AA625030,2001AA620503)NNSFC(Grant No.20432030)Key Innovative Project of the Academy(Grant No.KZCX3-SW-215).
文摘A novel method for the determination of cationic surfactant by laser thermal lens spectrometry was developed. It was based on the reaction between 1-hydroxy-2-(5-nitro-2-Pyri- dylazo)-8-aminonaphthalene-3,6-disulfonic acid (5-NO2-PAH) and cationic surfactant to form 1:2 ionic association complex in a weakly basic medium (pH 9.44). The determination conditions and the mechanism were discussed. The method has been applied to the analysis of wastewater and moat water samples.
文摘A novel phenolic glucoside was isolated from stem barks of Alangium plantanifolium, its structure was elucidated to be 1-O-[2-(1-hydroxy-6-oxocyclohex-2-ene-1-carboxymethyl) -phenyl]-4, 6-O-[(S)-4, 4', 5, 5', 6, 6'-hexahydroxydi-phenoyl]-beta -D-glucopyranose 1 by spectroscopic methods including 2D NMR techniques.
文摘This brief review discusses the behavioral consequences of two pharmacologically selected lines of rats. Flinders Sensitive (FSL) and Flinders Resistant (FRL) Lines of rats were selected on the basis of differential hypothermic and behavioral responses to the anticholinesterase, diisopropylfluorophosphate (DFP). FSL rats are more sensitive to the hypothermic effects of cholinergic, serotonergic, and dopaminergic agonists but less sensitive to the locomotor or stereotypic effects of dopamine agonists. FSL rats exhibit greater immobility in the forced swim test and reduced social interaction compared with FRL rats, but do not differ in saccharin intake, behavior in the elevated plus maze, or responses for rewarding brain self-stimulation. The exaggerated immobility and reduced social interaction are counteracted by chronic treatment with antidepressants. Because FSL rats were more sensitive to 5-HT1A receptor agonists, high (HDS) and low (LDS) 8-OH-DPATsensitive lines were selectively bred for differential hypothermic responses to the 5-HT1A receptor agonist, 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT). HDS rats were also more sensitive to the hypothermic effects of oxotremorine, a cholinergic agonist, but selection for this response did not diverge with later selection. HDS rats exhibited greater immobility in the forced swim test than LDS rats and this correlated response could be seen early in selection (generation 3). HDS rats also showed reduced social interaction compared to LDS rats, but did not differ in behavior in the elevated plus maze. These findings confirm that selection for hypothermic responses to pharmacological agents do have behavioral consequences, notably the production of depressive-like phenotypes, which can be counteracted by chronic antidepressant treatment. Because increased 5-HT1A receptor sensitivity was common to both selected lines (FSL and HDS), neurobiological processes dependent on this receptor could contribute to the abnormal behaviors that manifest in these rat lines and thus suggesting a mechanism underlying depressive behaviors in humans. However, available human data are inconsistent with this hypothesis and suggest that other mechanisms underlie these behavioral abnormalities in HDS and FSL rats. These mechanisms as well as additional behavioral testing in these rat lines will be discussed.
基金Financial support from the National Natural Science Foundation of China (NNSFCNos.81630094,81373287,and 30825044)
文摘Two pairs of unusual scalemic enantiomers with a dimethoxyphenyl)ethyl]-2-methoxyindolin-3-one, novel carbon skeleton of 2-[1′-(4"-hydroxy-3",5"- named isatidifoliumindolinones A-D (1-4), were isolated from an aqueous extract of lsatis indigotica leaves (da qing ye). Their structures including absolute configurations were determined by spectroscopic data analysis combined with comparison of their experimental CD and calculated ECD spectra. Validity of the ECD spectra calculation to assign the absolute configurations is discussed. Plausible biosynthetic pathways of 1-4 are proposed. Stereochemistry-dependent activity against LPS-induced NO production in BY2 cells was observed, and among the stereoisomers compound 4 is most active.
基金Supported by the National Natural Science Foundation of China (30170103).
文摘Two new isoflavonoid glucosides, 5-hydroxy-6,7-methylenedioxy-isoflavone-4'-O-D-glucopyranosyl (2→〉l)-L-rhamnoside (irilone-bioside) (compound 1) and 5,4'-methoxy-6,7-methylenedioxyisoflavone-3'-O-β-D-glucoside (irisleptophyllidin) (compound 2), together with five known compounds, nigricanin- 4'-O-β-D-glucoside (compound 3), irifloside (compound 4), irigenin (compound 5), 5, 3', 4'-trimethoxy-6,7-methylenedioxyisoflavone (compound 6), and nigricanin (compound 7) were isolated from the alcoholic extract of rhizomes of Iris leptophylla Lingelsh. Their structures were elucidated by spectroscopic methods.