A simple and concise approach for the synthesis of a series of new heterocyclic systems of 2-（benzofuran-2-yl）- benzo[h]quinoline-3-carboxylic acid derivatives （3a--3g） is described. The synthetic strategy feature...A simple and concise approach for the synthesis of a series of new heterocyclic systems of 2-（benzofuran-2-yl）- benzo[h]quinoline-3-carboxylic acid derivatives （3a--3g） is described. The synthetic strategy features the one-pot reaction of ethyl 2-（chloromethyl）benzo[h]quinoline-3-carboxylate （2） with various substituted salicylaldehydes as well as 2-hydroxy-l-naphthaldehyde as a key step. The substrate 2 was prepared in good yield by a mild, efficient and direct reaction of 1-naphthylamine （1） with Vilsmeier-Haack reagent. The structures of all the new compounds were identified by spectral data and elemental analysis.展开更多
The Al-doped Ni2P/AI-SBA-15 catalyst with high hydrodeoxygenation （HDO） activity was synthesized by tem- perature programmed reduction at a relatively low reduction temperature of 400 ℃. The as-prepared catalyst wa...The Al-doped Ni2P/AI-SBA-15 catalyst with high hydrodeoxygenation （HDO） activity was synthesized by tem- perature programmed reduction at a relatively low reduction temperature of 400 ℃. The as-prepared catalyst was characterized by X-ray diffraction （XRD）, H2 temperature-programmed reduction （H2-TPR）, X-ray photoelectron spectroscopy （XPS）, transmission electron microscope （TEM）, NH3 temperature programmed desorption （NH3-TPD）, N2 adsorption-desorption and CO uptake. The effect of AI on benzofuran （BF） HDO performance was investigated. The result indicates that the incorporation of AI into the SBA-15 support can promote the formation of much uniform, smaller, highly dispersed N2P particles on the catalyst. The AI also contrib- utes to suppress the enrichment of P and promote more exposed Ni sites on the surface. In addition, the incorporation of AI can enhance the acid strength. The total deoxygenated product yield over Ni2P/AI-SBA-15 reached 90.3%, which is an increase of 19.4%, when compared with that found for Ni2P/SBA-15 （70.9%）.展开更多
Two new benzofuran lignan glycosides, gelsemiunoside A and B, were isolated from the whole plant of Gelsemium elegans Benth. Their structures were elucidated on the basis of spectroscopic evidence. Furthermore, gelsem...Two new benzofuran lignan glycosides, gelsemiunoside A and B, were isolated from the whole plant of Gelsemium elegans Benth. Their structures were elucidated on the basis of spectroscopic evidence. Furthermore, gelsemiunoside A and B were shown a potent cytotoxic activity by suppressing the proliferation of A375-S2 cells.展开更多
Two new benzofuran derivatives were isolated from the roots of Ligularia stenocephala. Their structures were established by spectroscopic methods and 2D NMR experiments.
Objective:To find out the in vitro antipalsmodial activities of mangrove leaf extracts.Methods: In vitro antiplasmodial assay was carried out with 13 different mangrove plants.Column chromatography was performed with ...Objective:To find out the in vitro antipalsmodial activities of mangrove leaf extracts.Methods: In vitro antiplasmodial assay was carried out with 13 different mangrove plants.Column chromatography was performed with the most potent Agecerious corniculatum（A.corniculatum） by using various solvent extractions.GC-MS was also preformed with the most potent ethanolic fraction of the A.corniculatum extract.Results:Of the 13 mangroves plants, A.corniculatum showed maximum percentage of parasitemia suppression（94.98±1.16）%.Column chromatography was performed with A.corniculatum with different solvents and the methanolic extract showed maximum percentage（99.73±1.63）%of parasitemia inhibition at 150μg/mL concentration with the IC<sub>50</sub> value of（29.28±3.23）μg/mL concentration.The results of the GC-MS analysis observed that,the most potent methanolic extract showed maximum retention time（30.687 RT） and the chemical class was identified as Spiro[benzofuran-2（3 H）,1’-（3 cyclohexane）-2’,3- dione,7-chloro-4’,6]which was responsible for the antiplasmodial activity.Conclusions:It is concluded from the present study that,the chemical constituents of A.corniculatum collected from Pichavaram mangrove forest can be used as a putative antiplasmodial drugs in future.展开更多
A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H_(37)Rv and MDR-TB isolates as wel...A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H_(37)Rv and MDR-TB isolates as well as cytotoxicity. All benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids exhibited considerable in vitro anti-mycobacterial activities against the tested three MTB strains, and all of them also showed acceptable cytotoxicity. The most active hybrid 7f was >4.8 and >51 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H_(37)Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.展开更多
A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-（4-methoxyphenoxy）acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectro...A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-（4-methoxyphenoxy）acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectroscopy analysis including ^1H-NMR, ^13C-NMR, DEPT, ESI-MS, element analysis.展开更多
山豆根Sophorae Tonkinensis Radix et Rhizoma来源于豆科植物越南槐的干燥根和根茎,具有清热解毒、消肿利咽之功效,其化学成分复杂,药理活性多样。现代研究证明,山豆根中生物碱类、黄酮类、苯并呋喃类、三萜类、多糖类等化合物能抑制...山豆根Sophorae Tonkinensis Radix et Rhizoma来源于豆科植物越南槐的干燥根和根茎,具有清热解毒、消肿利咽之功效,其化学成分复杂,药理活性多样。现代研究证明,山豆根中生物碱类、黄酮类、苯并呋喃类、三萜类、多糖类等化合物能抑制肿瘤细胞的增殖、黏附、侵袭和转移,诱导细胞凋亡和自噬,抑制肿瘤血管生成,阻滞细胞周期和信号转导,还可通过提高机体免疫功能,抑制肿瘤的发生发展,对不同类型的恶性肿瘤均有良好的拮抗作用,具有多成分、多靶点、多通路的特点。通过对山豆根抗肿瘤活性成分及其作用机制进行综述,为山豆根抗肿瘤的深入研究和新药开发提供参考依据。展开更多
l-Methyl-3-ethyl imidazolium bromide[meim]Br/basic alumina（Al2O3） has been found to promote the cyclocondensation of chloroacetone/chloroethyl acetate with salicylaldehydes under conventional as well as microwave ir...l-Methyl-3-ethyl imidazolium bromide[meim]Br/basic alumina（Al2O3） has been found to promote the cyclocondensation of chloroacetone/chloroethyl acetate with salicylaldehydes under conventional as well as microwave irradiation to yield benzofuran derivatives.展开更多
The crystal structure of the potential active N-[2-(6-Methoxy-2-oxo-2H-chromen-4-yl)-benzofuran-3-yl]-benzamide (C25H17NO5) (I) has been determined from single crystal X-ray diffraction data. The title compound crysta...The crystal structure of the potential active N-[2-(6-Methoxy-2-oxo-2H-chromen-4-yl)-benzofuran-3-yl]-benzamide (C25H17NO5) (I) has been determined from single crystal X-ray diffraction data. The title compound crystallizes in the monoclinic space group P 21/n, with a = 12.0551(11), b = 9.7853(8), c = 16.6517(16) , β = 90.092(4)o, V = 1964.28(3) 3, Dcalc = 1.391 Mg/m3, Z = 4. In the structure, intermolecular H-bonds lead to the formation of a centrosymmetric dimer of the molecule. There is an intramolecular C7—H7…N1 hydrogen bond forming a closed seven membered ring. There are also intramolecular π-π interactions presented between the 3,6-Dihydro-2H-pyran ring of the chromen moiety [Cg2…Cg2 distance = 3.5812(13) ]. The packing structure is stabilized by these C—H…N, N—H…O hydrogen bonds, C—H… π and π…π interactions.展开更多
文摘A simple and concise approach for the synthesis of a series of new heterocyclic systems of 2-（benzofuran-2-yl）- benzo[h]quinoline-3-carboxylic acid derivatives （3a--3g） is described. The synthetic strategy features the one-pot reaction of ethyl 2-（chloromethyl）benzo[h]quinoline-3-carboxylate （2） with various substituted salicylaldehydes as well as 2-hydroxy-l-naphthaldehyde as a key step. The substrate 2 was prepared in good yield by a mild, efficient and direct reaction of 1-naphthylamine （1） with Vilsmeier-Haack reagent. The structures of all the new compounds were identified by spectral data and elemental analysis.
文摘The Al-doped Ni2P/AI-SBA-15 catalyst with high hydrodeoxygenation （HDO） activity was synthesized by tem- perature programmed reduction at a relatively low reduction temperature of 400 ℃. The as-prepared catalyst was characterized by X-ray diffraction （XRD）, H2 temperature-programmed reduction （H2-TPR）, X-ray photoelectron spectroscopy （XPS）, transmission electron microscope （TEM）, NH3 temperature programmed desorption （NH3-TPD）, N2 adsorption-desorption and CO uptake. The effect of AI on benzofuran （BF） HDO performance was investigated. The result indicates that the incorporation of AI into the SBA-15 support can promote the formation of much uniform, smaller, highly dispersed N2P particles on the catalyst. The AI also contrib- utes to suppress the enrichment of P and promote more exposed Ni sites on the surface. In addition, the incorporation of AI can enhance the acid strength. The total deoxygenated product yield over Ni2P/AI-SBA-15 reached 90.3%, which is an increase of 19.4%, when compared with that found for Ni2P/SBA-15 （70.9%）.
基金sponsored by the Scientific Research Foundation for the doctoral Scholars (Q.C.Zhao,No.20031040),Liaoning,China.
文摘Two new benzofuran lignan glycosides, gelsemiunoside A and B, were isolated from the whole plant of Gelsemium elegans Benth. Their structures were elucidated on the basis of spectroscopic evidence. Furthermore, gelsemiunoside A and B were shown a potent cytotoxic activity by suppressing the proliferation of A375-S2 cells.
文摘Two new benzofuran derivatives were isolated from the roots of Ligularia stenocephala. Their structures were established by spectroscopic methods and 2D NMR experiments.
基金Indian Council of Medical Research,New Dclhi for financial assistance
文摘Objective:To find out the in vitro antipalsmodial activities of mangrove leaf extracts.Methods: In vitro antiplasmodial assay was carried out with 13 different mangrove plants.Column chromatography was performed with the most potent Agecerious corniculatum（A.corniculatum） by using various solvent extractions.GC-MS was also preformed with the most potent ethanolic fraction of the A.corniculatum extract.Results:Of the 13 mangroves plants, A.corniculatum showed maximum percentage of parasitemia suppression（94.98±1.16）%.Column chromatography was performed with A.corniculatum with different solvents and the methanolic extract showed maximum percentage（99.73±1.63）%of parasitemia inhibition at 150μg/mL concentration with the IC<sub>50</sub> value of（29.28±3.23）μg/mL concentration.The results of the GC-MS analysis observed that,the most potent methanolic extract showed maximum retention time（30.687 RT） and the chemical class was identified as Spiro[benzofuran-2（3 H）,1’-（3 cyclohexane）-2’,3- dione,7-chloro-4’,6]which was responsible for the antiplasmodial activity.Conclusions:It is concluded from the present study that,the chemical constituents of A.corniculatum collected from Pichavaram mangrove forest can be used as a putative antiplasmodial drugs in future.
文摘A series of novel benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids were designed, synthesized and evaluated for their in vitro anti-TB activities against drug-sensitive MTB H_(37)Rv and MDR-TB isolates as well as cytotoxicity. All benzofuran-isatin-hydroxylimine/thiosemicarbazide hybrids exhibited considerable in vitro anti-mycobacterial activities against the tested three MTB strains, and all of them also showed acceptable cytotoxicity. The most active hybrid 7f was >4.8 and >51 folds more potent than the first line anti-TB agents RIF and INH against both drug-sensitive MTB H_(37)Rv and MDR-TB isolates, respectively. The results demonstrated the potential utility of benzofuran-isatin-hydroxylimine/-thiosemicarbazide hybrids as anti-TB agents.
基金supported by the National Natural Science Foundation of China(20472117,20272085)the Natural Science Foundation of Guangdong Province(031594).
文摘A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-（4-methoxyphenoxy）acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectroscopy analysis including ^1H-NMR, ^13C-NMR, DEPT, ESI-MS, element analysis.
文摘山豆根Sophorae Tonkinensis Radix et Rhizoma来源于豆科植物越南槐的干燥根和根茎,具有清热解毒、消肿利咽之功效,其化学成分复杂,药理活性多样。现代研究证明,山豆根中生物碱类、黄酮类、苯并呋喃类、三萜类、多糖类等化合物能抑制肿瘤细胞的增殖、黏附、侵袭和转移,诱导细胞凋亡和自噬,抑制肿瘤血管生成,阻滞细胞周期和信号转导,还可通过提高机体免疫功能,抑制肿瘤的发生发展,对不同类型的恶性肿瘤均有良好的拮抗作用,具有多成分、多靶点、多通路的特点。通过对山豆根抗肿瘤活性成分及其作用机制进行综述,为山豆根抗肿瘤的深入研究和新药开发提供参考依据。
文摘l-Methyl-3-ethyl imidazolium bromide[meim]Br/basic alumina（Al2O3） has been found to promote the cyclocondensation of chloroacetone/chloroethyl acetate with salicylaldehydes under conventional as well as microwave irradiation to yield benzofuran derivatives.
文摘The crystal structure of the potential active N-[2-(6-Methoxy-2-oxo-2H-chromen-4-yl)-benzofuran-3-yl]-benzamide (C25H17NO5) (I) has been determined from single crystal X-ray diffraction data. The title compound crystallizes in the monoclinic space group P 21/n, with a = 12.0551(11), b = 9.7853(8), c = 16.6517(16) , β = 90.092(4)o, V = 1964.28(3) 3, Dcalc = 1.391 Mg/m3, Z = 4. In the structure, intermolecular H-bonds lead to the formation of a centrosymmetric dimer of the molecule. There is an intramolecular C7—H7…N1 hydrogen bond forming a closed seven membered ring. There are also intramolecular π-π interactions presented between the 3,6-Dihydro-2H-pyran ring of the chromen moiety [Cg2…Cg2 distance = 3.5812(13) ]. The packing structure is stabilized by these C—H…N, N—H…O hydrogen bonds, C—H… π and π…π interactions.
