A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus(HBV) activity and cytotoxicity in HepG2.2.15 cells.Half of the tested compounds were found to be potent agai...A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus(HBV) activity and cytotoxicity in HepG2.2.15 cells.Half of the tested compounds were found to be potent against HBsAg secretion with IC50 values less than 100μmol/L.Compounds 14c,14d,and 14e showed significant inhibitory activity to the viral antigen HBeAg.展开更多
acetoxy-17,17-ethylendioxy-15β,16β-methylene-5-androsten-7β-ol（Ⅰ） was prepared by 3 steps from 3β-acetoxy-15β,16β-methylene-5-androsten-17-one （Ⅱ） with overall yield of 52.7%. Thus, interaction of ethylene...acetoxy-17,17-ethylendioxy-15β,16β-methylene-5-androsten-7β-ol（Ⅰ） was prepared by 3 steps from 3β-acetoxy-15β,16β-methylene-5-androsten-17-one （Ⅱ） with overall yield of 52.7%. Thus, interaction of ethylene glycol and material （Ⅱ） gave 3β-acetoxy- 17,17-ethylendioxy-15β,16β-methylene-5-androsten （Ⅲ） which was subsequently oxidated and stereoselectively reduced to produce compound（Ⅰ）. The normal influencing factors, such as the types of oxidants and reductives, the mole ratio of reactants, the reaction temperature, and the addition ways of reactants, in oxidation and reduction were discussed. The results show that the oxidation rate order is CrO3-C5H5N （1∶1, mole fraction）>CrO3-C5H5N（1∶2）>（C5H5NH）2Cr2O7 in terms of the oxidant, the yield of the oxidation becomes higher with increasing the oxidant stoichiometry and raising the reaction temperature. And the optimum condition is that the reaction temperature is at 30 ℃, and n （Ⅲ）/ n （CrO3-C5H5N（1∶2））=1∶20. The yield of the -7β alcohol order with Li[Al（OC（CH3）3）3H] （e.g.78.6%） is more than that with NaBH4 （e.g.14.5%） in terms of the reductive （agent） and the reduction rate decreases in the course of reaction. The compound （Ⅰ） is characterized by IR and MS.展开更多
采用硅胶柱色谱、凝胶色谱及高压制备色谱等方法对滇重楼[Paris polyphylla Smith var.yunnanensis(Franch.)Hand.-Mazz.]根茎部位进行分离纯化。共分离得到10个化合物,分别是棕榈酸(1),pinnatasterone(2),胸苷(3),20-hydroxyecdysone(...采用硅胶柱色谱、凝胶色谱及高压制备色谱等方法对滇重楼[Paris polyphylla Smith var.yunnanensis(Franch.)Hand.-Mazz.]根茎部位进行分离纯化。共分离得到10个化合物,分别是棕榈酸(1),pinnatasterone(2),胸苷(3),20-hydroxyecdysone(4),腺嘌呤核苷(5),偏诺皂苷元-3-O-α-L-鼠李吡喃糖(1→2)-[α-L-阿拉伯呋喃糖(1→4)]-β-D-葡萄吡喃糖苷(6),bis(2-ethylhexyl)benzene-1,2-dicarboxylate(7),薯蓣皂苷(8),2-O-β-D-fructofuranosyl-α-D-allopyranose(9),n-tritetracontan-5α-ol(10)。其中,化合物9为首次从该植物中分离得到,化合物7,10为首次从该植物属中分离得到。展开更多
Based upon the crystal structure of a previously reported fragment hit that binds to Corresponding author. β-secretase, a novel series of non-peptidic small-molecule β-secretase inhibitors, namely hexahydropyrimidin...Based upon the crystal structure of a previously reported fragment hit that binds to Corresponding author. β-secretase, a novel series of non-peptidic small-molecule β-secretase inhibitors, namely hexahydropyrimidin-5-ols, along with two series of their analogues, were rationally designed through structural modification. The CADD study was performed and revealed good expectation. Inhibitory activities of the corresponding structural cores were tested, which provided further support for our design approach.展开更多
A series of novel bispyrazoles joined by arylmethylene at C-4 position were synthesized with aromatic aldehydes obtained from lignin and screened for their in vitro antioxidant activities by N,N-diphenyl-N＇picrylhydr...A series of novel bispyrazoles joined by arylmethylene at C-4 position were synthesized with aromatic aldehydes obtained from lignin and screened for their in vitro antioxidant activities by N,N-diphenyl-N＇picrylhydrazyl （DPPH） and 2,2＇-azino-bis（3-ethylenzothiazoline-sulphonic acid） diammonium salt （ABTS＋） radical scavenging assays. All of these compounds exhibited good DPPH and ABST＋ radical scavenging activities as compared to the standard, Trolox, which suggested their potential as promising agents for cturing tumors or other free radical-related diseases.展开更多
2-[3,5-Di-O-β-D-glucosyl-4-(3-methylbut-2-enyl)phenyl]benzofuran-6-ol,a new prenylated arylbenzofuran derivative was isolated from Morus alba L.Its structure was elucidated by various spectroscopic methods including ...2-[3,5-Di-O-β-D-glucosyl-4-(3-methylbut-2-enyl)phenyl]benzofuran-6-ol,a new prenylated arylbenzofuran derivative was isolated from Morus alba L.Its structure was elucidated by various spectroscopic methods including MS,~1H NMR,^(13)C NMR,DEPT,~1H-~1HCOSY,HMQC and HMBC.展开更多
N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performan...N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performance were also studied. The results show that this ionic liquid is an excellent catalyst for the synthesis of 4,4＇-（arylmethylene）bis（1H-pyrazol-5-ol） derivatives under solvent-free conditions.This method has the advantages of high yield, clean transformation, simple operation and short reaction time. The ionic liquid can be recycled without significant loss of activity.展开更多
Phytochemical investigation of the purified fractions of the active dichloromethane extract of Hysterionica pinifolia (Poir.) Baker led to the identification of five compounds. New acetylenic alcohol (E)-undec-3-en-5,...Phytochemical investigation of the purified fractions of the active dichloromethane extract of Hysterionica pinifolia (Poir.) Baker led to the identification of five compounds. New acetylenic alcohol (E)-undec-3-en-5,7-diyne-1-ol (1) and three other compounds (3), (4), and (5) were reported for the first time in this species. Furthermore, forty-six components from the volatile fraction of H. pinifolia were identified. These compounds were elucidated using 1D and 2D NMR spectroscopy as well as MS-ESI and GC-FID-MS experiments. The dichloromethane extract, its fractions, and the methanolic extract were tested for insecticidal activity against Tribolium castaneum under laboratory conditions. The dichloromethane extract and the fraction F2 were found to be active, showing high larval mortality. The dichloromethane extract was also active against T. castaneum adults. The results have shown that H. pinifolia could be considered, in a near future, as a potential source for the development of a botanical insecticide for pest control.展开更多
Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by si...Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by silica gel column chromatography and preparative HPLC.The structures of the isolated compounds were identified by spectral analyses,physical constants,and chemical evidences.Results Two cucurbitane triterpenoids were isolated and identified as 5β,19-epoxy-cucurbita-6,22E,24-trien-3β-ol(1)and cucurbita-6,22(E),24-trien-3β-ol-19,5β-olide(2).Conclusion Compound 1 is a new compound.展开更多
文摘A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus(HBV) activity and cytotoxicity in HepG2.2.15 cells.Half of the tested compounds were found to be potent against HBsAg secretion with IC50 values less than 100μmol/L.Compounds 14c,14d,and 14e showed significant inhibitory activity to the viral antigen HBeAg.
文摘acetoxy-17,17-ethylendioxy-15β,16β-methylene-5-androsten-7β-ol（Ⅰ） was prepared by 3 steps from 3β-acetoxy-15β,16β-methylene-5-androsten-17-one （Ⅱ） with overall yield of 52.7%. Thus, interaction of ethylene glycol and material （Ⅱ） gave 3β-acetoxy- 17,17-ethylendioxy-15β,16β-methylene-5-androsten （Ⅲ） which was subsequently oxidated and stereoselectively reduced to produce compound（Ⅰ）. The normal influencing factors, such as the types of oxidants and reductives, the mole ratio of reactants, the reaction temperature, and the addition ways of reactants, in oxidation and reduction were discussed. The results show that the oxidation rate order is CrO3-C5H5N （1∶1, mole fraction）>CrO3-C5H5N（1∶2）>（C5H5NH）2Cr2O7 in terms of the oxidant, the yield of the oxidation becomes higher with increasing the oxidant stoichiometry and raising the reaction temperature. And the optimum condition is that the reaction temperature is at 30 ℃, and n （Ⅲ）/ n （CrO3-C5H5N（1∶2））=1∶20. The yield of the -7β alcohol order with Li[Al（OC（CH3）3）3H] （e.g.78.6%） is more than that with NaBH4 （e.g.14.5%） in terms of the reductive （agent） and the reduction rate decreases in the course of reaction. The compound （Ⅰ） is characterized by IR and MS.
文摘采用硅胶柱色谱、凝胶色谱及高压制备色谱等方法对滇重楼[Paris polyphylla Smith var.yunnanensis(Franch.)Hand.-Mazz.]根茎部位进行分离纯化。共分离得到10个化合物,分别是棕榈酸(1),pinnatasterone(2),胸苷(3),20-hydroxyecdysone(4),腺嘌呤核苷(5),偏诺皂苷元-3-O-α-L-鼠李吡喃糖(1→2)-[α-L-阿拉伯呋喃糖(1→4)]-β-D-葡萄吡喃糖苷(6),bis(2-ethylhexyl)benzene-1,2-dicarboxylate(7),薯蓣皂苷(8),2-O-β-D-fructofuranosyl-α-D-allopyranose(9),n-tritetracontan-5α-ol(10)。其中,化合物9为首次从该植物中分离得到,化合物7,10为首次从该植物属中分离得到。
基金National Natural Science Foundation of China (Grant No.20772008 and 30772650)
文摘Based upon the crystal structure of a previously reported fragment hit that binds to Corresponding author. β-secretase, a novel series of non-peptidic small-molecule β-secretase inhibitors, namely hexahydropyrimidin-5-ols, along with two series of their analogues, were rationally designed through structural modification. The CADD study was performed and revealed good expectation. Inhibitory activities of the corresponding structural cores were tested, which provided further support for our design approach.
文摘A series of novel bispyrazoles joined by arylmethylene at C-4 position were synthesized with aromatic aldehydes obtained from lignin and screened for their in vitro antioxidant activities by N,N-diphenyl-N＇picrylhydrazyl （DPPH） and 2,2＇-azino-bis（3-ethylenzothiazoline-sulphonic acid） diammonium salt （ABTS＋） radical scavenging assays. All of these compounds exhibited good DPPH and ABST＋ radical scavenging activities as compared to the standard, Trolox, which suggested their potential as promising agents for cturing tumors or other free radical-related diseases.
基金supported by the Great Research Project of National Major New Drug Development(No. 2009ZX09102-110)
文摘2-[3,5-Di-O-β-D-glucosyl-4-(3-methylbut-2-enyl)phenyl]benzofuran-6-ol,a new prenylated arylbenzofuran derivative was isolated from Morus alba L.Its structure was elucidated by various spectroscopic methods including MS,~1H NMR,^(13)C NMR,DEPT,~1H-~1HCOSY,HMQC and HMBC.
基金the partial support from University Malaya to Project GC 001A-14-AET
文摘N-Methylimidazolium perchlorate（[MIm]ClO_4） was synthesized and some of its physico-chemical properties, such as density, surface tension were investigated. A thermo gravimetric analysis（TGA） and solvent performance were also studied. The results show that this ionic liquid is an excellent catalyst for the synthesis of 4,4＇-（arylmethylene）bis（1H-pyrazol-5-ol） derivatives under solvent-free conditions.This method has the advantages of high yield, clean transformation, simple operation and short reaction time. The ionic liquid can be recycled without significant loss of activity.
文摘Phytochemical investigation of the purified fractions of the active dichloromethane extract of Hysterionica pinifolia (Poir.) Baker led to the identification of five compounds. New acetylenic alcohol (E)-undec-3-en-5,7-diyne-1-ol (1) and three other compounds (3), (4), and (5) were reported for the first time in this species. Furthermore, forty-six components from the volatile fraction of H. pinifolia were identified. These compounds were elucidated using 1D and 2D NMR spectroscopy as well as MS-ESI and GC-FID-MS experiments. The dichloromethane extract, its fractions, and the methanolic extract were tested for insecticidal activity against Tribolium castaneum under laboratory conditions. The dichloromethane extract and the fraction F2 were found to be active, showing high larval mortality. The dichloromethane extract was also active against T. castaneum adults. The results have shown that H. pinifolia could be considered, in a near future, as a potential source for the development of a botanical insecticide for pest control.
基金National New Drug Incubation(Benxi)Base Construction of Liaoning Province(2010ZX09401-304-105B)the Doctoral InitiatingFoundation Project of Liaoning Province(20101108)
文摘Objective To study the chemical constituents in the acid-hydrolyzed ethanol extract from Momordica charantia.Methods The ethanol extract from M.charantia was hydrolyzed by 36%HCl and the hydrolysate was isolated by silica gel column chromatography and preparative HPLC.The structures of the isolated compounds were identified by spectral analyses,physical constants,and chemical evidences.Results Two cucurbitane triterpenoids were isolated and identified as 5β,19-epoxy-cucurbita-6,22E,24-trien-3β-ol(1)and cucurbita-6,22(E),24-trien-3β-ol-19,5β-olide(2).Conclusion Compound 1 is a new compound.
