Entecavir can significantly inhibit the replication of HBV-DNA, reduce the HBV-DNA level in blood se- rum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor meta-...Entecavir can significantly inhibit the replication of HBV-DNA, reduce the HBV-DNA level in blood se- rum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor meta- bolic 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-HBV activities with that of entecavir, especially.展开更多
This article is retracted because the corresponding author XU Youjun was put as the corresponding author without knowing anything before its publication. All were arranged by the first author, Mr. FENG Deri, in abnorm...This article is retracted because the corresponding author XU Youjun was put as the corresponding author without knowing anything before its publication. All were arranged by the first author, Mr. FENG Deri, in abnormal ways. Hence all other authors and XU state here that this paper has no relation with other authors and with Xu＇s working university. XU also states that he has never used ＂xuyoujun65@163.com＂as corresponding author contact email.展开更多
基金Supported by the National Natural Science Foundation of China（No.51209024） and the Science and Technology Plan of Si- chuan Province, China（No.2010JY0122）.
文摘Entecavir can significantly inhibit the replication of HBV-DNA, reduce the HBV-DNA level in blood se- rum. But suffering from low oral bioavailability, entecavir has low intestinal membrane permeability and poor meta- bolic 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-HBV activities with that of entecavir, especially.
文摘This article is retracted because the corresponding author XU Youjun was put as the corresponding author without knowing anything before its publication. All were arranged by the first author, Mr. FENG Deri, in abnormal ways. Hence all other authors and XU state here that this paper has no relation with other authors and with Xu＇s working university. XU also states that he has never used ＂xuyoujun65@163.com＂as corresponding author contact email.
