摘要
以阿昔洛韦和琥珀酸酐为原料,100 mL DMF为反应媒介,加入0.7 mL三乙胺,合成琥珀酰阿昔洛韦[9-(2-丁二酸单酰乙氧基甲基)鸟嘌呤](SACV),然后利用Fmoc固相合成法合成三个新的阿昔洛韦二肽衍生物(SACV-Glu-Lys,SACV-Glu-Ala,SACV-Val-Lys).利用1H NMR和ESI-MS分析手段对其结构进行表征.并考察了二肽修饰过的阿昔洛韦,水溶性,油脂分配系数.结果表明含有较长的侧链酸性氨基酸与碱性氨基酸形成的二肽所修饰阿昔洛韦,既可以较大的提高阿昔洛韦(ACV)的水溶性又能够得到油水分配系数较高的ACV二肽衍生物.
Succinyl acyclovir （SACV） was prepared by acyclovir coupled with succinic anhydride as materials and 100 mL DMF as the reaction medium, adding 0.7 mL of triethylamine. Then three new aeyclovir dipeptide derivatives SACV-GIu-Lys, SACV-GIu-Ala and SACV-Val-Lys were synthesized by Fmoc solid synthesis method. The structures of SACV and three new acyclovir dipeptide derivatives were characterized by 1H NMR and ESI-MS, water-solubility and oil partition coefficient of the dipeptide modified aeyelovir were also investigated. The results showed that dipeptide modified aeyclovir was achieved with the use of acidic amino acid and alkaline amino acid containing longer side chains, its water-solubility was greatly improved and oil-water partition coefficient of the ACV dipeptide derivatives was also increased.
出处
《河南科学》
2014年第5期711-715,共5页
Henan Science
基金
国家自然科学基金(21172054)
河南省创新型科技人才队伍建设工程(104200510022)
