Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with...Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC50 values of sub μmol/L level. The ICso of anti-HBsAg activities of 5c and 5j reached 0.01 μmol/L respectively which were 16 fold more potent than that of 3TC. Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg. The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents.展开更多
The glycosylation of hydroxylcoumarin was investigated by using suspension cultures of hairy roots of Polygonum multiflorum. Two new coumarin glucosides （3 and 4） were biosysthesized by regioselectively glycosylatio...The glycosylation of hydroxylcoumarin was investigated by using suspension cultures of hairy roots of Polygonum multiflorum. Two new coumarin glucosides （3 and 4） were biosysthesized by regioselectively glycosylation of corresponding substrates （1 and 2） in the system. The structures of two products were identified as 7-hydroxy-4-methylcoumarin 5-O-β-D-glucopyranoside and 7- hydroxy-3,4-dimethylcoumarin 5-O-β-D-glucopyranoside on the ground of chemical and spectroscopic methods, respectively. 2007 Rong Min Yu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
A new chemiluminescent reagent 7-(4,6-dichloro-1,3,5-triazinylamino)-4-methylcoumarin-4-methylcoumarin (DTMC) was synthesized by linking 7-amino-4-methylcoumarin to cyanuric chloride at 0-5 degreesC, and with it a nov...A new chemiluminescent reagent 7-(4,6-dichloro-1,3,5-triazinylamino)-4-methylcoumarin-4-methylcoumarin (DTMC) was synthesized by linking 7-amino-4-methylcoumarin to cyanuric chloride at 0-5 degreesC, and with it a novel chemiluminescence method was developed for the determination of hydrogen peroxide. The selectivity of this method is high, and most of the transition metal ions have no effect on the determination of H2O2.展开更多
Monomer of 7-methacryloyloxy-4-methylcoumarin （MAOMC） was synthesized and characterized by FTIR, 1H-NMR and 13C-NMR spectroscopy. Copolymers of MAOMC with butoxyethylmethacrylate （BOEMA） at different feed composit...Monomer of 7-methacryloyloxy-4-methylcoumarin （MAOMC） was synthesized and characterized by FTIR, 1H-NMR and 13C-NMR spectroscopy. Copolymers of MAOMC with butoxyethylmethacrylate （BOEMA） at different feed compositions were prepared by free radical solution polymerization at （70 ± 1） ℃ in ethylmethylketonc （EMK） using benzyl peroxide （BPO） as an initiator. The copolymers were characterized by FTIR and IH-NMR spectroscopy. Thermogravimetric analysis （TGA） and differential scanning calorimetry （DSC） of the copolymers showed moderate thermal stability and higher Tg values. Gel permeation chromatography （GPC） was used to find out the molecular weights of the different copolymers. Antibacterial activities of the copolymers were also investigated against the selected pathogenic bacteria＇s. The antibacterial activity of the copolymer increases as the MAOMC content increases in the copolymer. This shows that coumarin moiety plays a very important role in the antibacterial activity.展开更多
基金a grant from National Science Foundation of China(No.20272010 and 30200348)awarded to P.Xia and Y.Chert,respectively.
文摘Twelve S-substituted 7-mercapto-4-methylcoumarin analogs were synthesized and evaluated for the inhibition to HBV in HepG2 2.2.1.5 cell. Among them, ten compounds exhibited potent inhibition to HBsAg and/or HBeAg with the IC50 values of sub μmol/L level. The ICso of anti-HBsAg activities of 5c and 5j reached 0.01 μmol/L respectively which were 16 fold more potent than that of 3TC. Compounds 3, 5e, 5g, 5h and 5i showed admirable inhibitory activity to both HBsAg and HBeAg. The bioassay results indicated the S-substituted 7-mercapto-4-methylcoumarin analogs merit attention as novel anti-HBV agents.
文摘The glycosylation of hydroxylcoumarin was investigated by using suspension cultures of hairy roots of Polygonum multiflorum. Two new coumarin glucosides （3 and 4） were biosysthesized by regioselectively glycosylation of corresponding substrates （1 and 2） in the system. The structures of two products were identified as 7-hydroxy-4-methylcoumarin 5-O-β-D-glucopyranoside and 7- hydroxy-3,4-dimethylcoumarin 5-O-β-D-glucopyranoside on the ground of chemical and spectroscopic methods, respectively. 2007 Rong Min Yu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
基金the Alexander von Humboldt Foundation of Germany, the National Natural Science Foundation of China, CAS (KJ951-A1-507) and presi
文摘A new chemiluminescent reagent 7-(4,6-dichloro-1,3,5-triazinylamino)-4-methylcoumarin-4-methylcoumarin (DTMC) was synthesized by linking 7-amino-4-methylcoumarin to cyanuric chloride at 0-5 degreesC, and with it a novel chemiluminescence method was developed for the determination of hydrogen peroxide. The selectivity of this method is high, and most of the transition metal ions have no effect on the determination of H2O2.
文摘Monomer of 7-methacryloyloxy-4-methylcoumarin （MAOMC） was synthesized and characterized by FTIR, 1H-NMR and 13C-NMR spectroscopy. Copolymers of MAOMC with butoxyethylmethacrylate （BOEMA） at different feed compositions were prepared by free radical solution polymerization at （70 ± 1） ℃ in ethylmethylketonc （EMK） using benzyl peroxide （BPO） as an initiator. The copolymers were characterized by FTIR and IH-NMR spectroscopy. Thermogravimetric analysis （TGA） and differential scanning calorimetry （DSC） of the copolymers showed moderate thermal stability and higher Tg values. Gel permeation chromatography （GPC） was used to find out the molecular weights of the different copolymers. Antibacterial activities of the copolymers were also investigated against the selected pathogenic bacteria＇s. The antibacterial activity of the copolymer increases as the MAOMC content increases in the copolymer. This shows that coumarin moiety plays a very important role in the antibacterial activity.
