RETRACTED: Synthesis and Biological Evaluation of Entecavir 4′-Ester Derivatives (Retracted article. See vol. 31, pg. 1078, 2015)

被引：3

作者：

Feng Deri ^{[1
]}

Liu Jiaan ^{[1
]}

Liang Shuang ^{[1
]}

Wang Yanyan ^{[1
]}

Xu Youjun ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2014年 / 30卷 / 05期

基金：

中国国家自然科学基金;

关键词：

Entecavir; Anti-HBV activity; Intestinal membrane permeability; HEPATITIS-B-VIRUS; PHARMACOKINETICS; INFECTION; PRODRUG; POTENT; ACID; LAMIVUDINE; TRIAL; DRUG;

D O I：

10.1007/s40242-014-4183-y

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Entecavir can significantly inhibit the replication of HBV-DNA, reduce the HBV-DNA level in blood serum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor metabolic stability. In this study, 12 different derivatives of entecavir 4'-ester were regioselectively synthesized and their apical-to-basolateral permeabilities across Caco-2 cells and HBV-DNA inhibitory efficacies were evaluated. Most of the compounds showed high permeabilities across Caco-2 cells compared with entecavir, compounds 5b and 5e also exhibited comparable anti-BBV activities with that of entecavir, especially.

引用

页码：749 / 754

页数：6

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