【摘 要】
：
Acyclovir (9-(2-hydroxyethoxymethyl) guanine) with a low bioavailability is an acyclic nucleoside analogue that has shown a potent antiviral activity.L-Fuco
【机 构】
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InstituteofBiologicalSciences&Biotechnology,DonghuaUniversity,2999NorthRenminRoad,Shanghai,201620,Ch
【出 处】
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2007 Enzyme Engineering Conference(国际酶工程学术会议)
论文部分内容阅读
Acyclovir (9-(2-hydroxyethoxymethyl) guanine) with a low bioavailability is an acyclic nucleoside analogue that has shown a potent antiviral activity.L-Fucose,the main monosaccharide of Fucoidan has anticoagulant,antitumor,and anti-HIV activities.To improve the bioavailability and antiviral activity of acyclovir,a controllable high regioselective enzymatic synthesis approach for the preparation of acyclovir vinyl derivative with L-fucose was developed.Firstly,transesterification of acyclovir with divinyl dicarboxylates was performed under the catalysis of protease from Bacillus subtilis in anhydrous pyridine at 50℃.O-acylacyclovir derivative was obtained successfully.And then,protease-catalyzed high regionselective acylation of L-fucose with vinyl ester of acyclovir gave drug-saccharine derivative.The obtained polymeric prodrug was characterized with IR,NMR,GPC.The biodegradation of the drug-saccharine derivative was investigated using enzymatic method in aqueous buffer,and result showed that the polymer was biodegradable.
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