A novel tripodal receptor,1,3,5-tri((5,7-dimethyl-1,8-naphthyridin-2-yl-amino)methyl)-2,4,6-triethylbenzene(1) was synthesized from starting materials 2,6-diamino-pyridine(2) and 1,3,5-triethylbenzene(4) by three step...A novel tripodal receptor,1,3,5-tri((5,7-dimethyl-1,8-naphthyridin-2-yl-amino)methyl)-2,4,6-triethylbenzene(1) was synthesized from starting materials 2,6-diamino-pyridine(2) and 1,3,5-triethylbenzene(4) by three steps with an overall yield of 25%,and characterized by ESI-MS,FT-IR and ~1H NMR spectra.Additionally,its absorption and emission spectra were investigated.展开更多
A simple and regioselective synthesis of 2-chloro-3-formyl-l,8-naphthyridine （1） through V ilsmeier-Haack cyclization of N-（pyridine-2-yl） acetamide has been reported. The reaction of compound （1） with sodium su...A simple and regioselective synthesis of 2-chloro-3-formyl-l,8-naphthyridine （1） through V ilsmeier-Haack cyclization of N-（pyridine-2-yl） acetamide has been reported. The reaction of compound （1） with sodium sulphide gives thione （2） and the reaction of compound （1） with Na2S/DMF followed by reaction with alkyl halide in one pot afforded thioether （3 and 4）. New naphthyridone （5） was synthesized from the action of acetic acid and POCI3 in compound （1）. The condensation of compounds （1 and 8） with hydroxylamine and aniline leads to the formation of compounds （6, 7 and 9）. The 2-chloro-3-formyl-l,8-naphthyridine was treated with sodium azide underwent cyclization to afford tetrazolo （l,5-a） （l,8-naphthyridine-4-carbaldehyde （8）. The azitidinone （10 and 12） and thioazolidinone （11 and 13） were synthesized from shift base intermediates by using chloroacetyl chloride and thioglycolic acid. The formyl group in compound （1） is subjected to cyano （14） and 3-alkoxycarbonyl （15）, respectively. The ester （15） was treated with hydrazine hydrate in ethanol to give acid hydrazide （16） then converted to thio semicarbazide （17） by their reaction with ammonium thiocyanate. New thiadiazolo （18）, triazolo （19） and oxadiazolo （20） have been prepared. The structures of synthesized compounds have been confirmed by suitable spectroscopic techniques such as IR （infrared spectrometry） and ^1H NMR （proton nuclear magnetic resonance）.展开更多
The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the...The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the excretion of bile acids,thus increasing bile acid synthesis and consequently cholesterol consumption.Therefore,ASBT is an attractive target for developing new cholesterol-lowering drugs.In this report,a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT.Most of them demonstrated potency against ASBT transport of bile acids.In particular,compound 4a_1 was found to have the best activity,resulting in 80.1%inhibition of ASBT at10μmol/L.展开更多
Di（2-amino-5-methyl-1,8-naphthyridin-1-ium-7-carboxylato）dichlorocuprate（Ⅱ） di- hydrate has been prepared from 5,7-dimethyl-1,8-naphthyridine-2-amine, CuCl2·2H2O and concentrated hydrochloride acid, and its ...Di（2-amino-5-methyl-1,8-naphthyridin-1-ium-7-carboxylato）dichlorocuprate（Ⅱ） di- hydrate has been prepared from 5,7-dimethyl-1,8-naphthyridine-2-amine, CuCl2·2H2O and concentrated hydrochloride acid, and its structure was determined by X-ray diffraction at 298 K. The compound （C20H22Cl2CuN6O6, Mr = 576.88） crystallizes in monoclinic, space group P21/n with a = 9.102（9）, b = 12.150（12）, c = 10.619（10） A,β = 91.20°, V= 1174.1（19） A^3, Z= 2, Dc= 1.632 g/cm^3, F（000） = 590,μ = 1.208 mm^-1, R = 0.0392 and wR = 0.0984. The Cu^2＋ ion is six-coordinated by two nitrogen and two oxygen atoms from two different naphthyridine ligands at the equatorial positions together with two chloride ions located at the axial positions.展开更多
基金the National Natural Science Foundation of China(Nos.20671094 and 90610034)the foundation (No.GJHZ05) for Bureau of International Co-operation of Chinese Academy of Science.
文摘A novel tripodal receptor,1,3,5-tri((5,7-dimethyl-1,8-naphthyridin-2-yl-amino)methyl)-2,4,6-triethylbenzene(1) was synthesized from starting materials 2,6-diamino-pyridine(2) and 1,3,5-triethylbenzene(4) by three steps with an overall yield of 25%,and characterized by ESI-MS,FT-IR and ~1H NMR spectra.Additionally,its absorption and emission spectra were investigated.
文摘A simple and regioselective synthesis of 2-chloro-3-formyl-l,8-naphthyridine （1） through V ilsmeier-Haack cyclization of N-（pyridine-2-yl） acetamide has been reported. The reaction of compound （1） with sodium sulphide gives thione （2） and the reaction of compound （1） with Na2S/DMF followed by reaction with alkyl halide in one pot afforded thioether （3 and 4）. New naphthyridone （5） was synthesized from the action of acetic acid and POCI3 in compound （1）. The condensation of compounds （1 and 8） with hydroxylamine and aniline leads to the formation of compounds （6, 7 and 9）. The 2-chloro-3-formyl-l,8-naphthyridine was treated with sodium azide underwent cyclization to afford tetrazolo （l,5-a） （l,8-naphthyridine-4-carbaldehyde （8）. The azitidinone （10 and 12） and thioazolidinone （11 and 13） were synthesized from shift base intermediates by using chloroacetyl chloride and thioglycolic acid. The formyl group in compound （1） is subjected to cyano （14） and 3-alkoxycarbonyl （15）, respectively. The ester （15） was treated with hydrazine hydrate in ethanol to give acid hydrazide （16） then converted to thio semicarbazide （17） by their reaction with ammonium thiocyanate. New thiadiazolo （18）, triazolo （19） and oxadiazolo （20） have been prepared. The structures of synthesized compounds have been confirmed by suitable spectroscopic techniques such as IR （infrared spectrometry） and ^1H NMR （proton nuclear magnetic resonance）.
基金supported by the National Natural Science Foundation of China(Nos.81473098 and 81473099)Hebei Provincial Key Research Project of Medical Science(Nos.ZD20140027 and 20150588)
文摘The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the excretion of bile acids,thus increasing bile acid synthesis and consequently cholesterol consumption.Therefore,ASBT is an attractive target for developing new cholesterol-lowering drugs.In this report,a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT.Most of them demonstrated potency against ASBT transport of bile acids.In particular,compound 4a_1 was found to have the best activity,resulting in 80.1%inhibition of ASBT at10μmol/L.
基金the Natural Science Foundation of Zhejiang Province
文摘Di（2-amino-5-methyl-1,8-naphthyridin-1-ium-7-carboxylato）dichlorocuprate（Ⅱ） di- hydrate has been prepared from 5,7-dimethyl-1,8-naphthyridine-2-amine, CuCl2·2H2O and concentrated hydrochloride acid, and its structure was determined by X-ray diffraction at 298 K. The compound （C20H22Cl2CuN6O6, Mr = 576.88） crystallizes in monoclinic, space group P21/n with a = 9.102（9）, b = 12.150（12）, c = 10.619（10） A,β = 91.20°, V= 1174.1（19） A^3, Z= 2, Dc= 1.632 g/cm^3, F（000） = 590,μ = 1.208 mm^-1, R = 0.0392 and wR = 0.0984. The Cu^2＋ ion is six-coordinated by two nitrogen and two oxygen atoms from two different naphthyridine ligands at the equatorial positions together with two chloride ions located at the axial positions.
