一种具有显著抗病毒活性的胸苷磷酸化酶稳定的BVDU类似物。
A thymidine phosphorylase-stable analogue of BVDU with significant antiviral activity.
作者信息
Guenther Sven, Balzarini Jan, De Clercq Erik, Nair Vasu
机构信息
Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602, USA.
出版信息
J Med Chem. 2002 Dec 5;45(25):5426-9. doi: 10.1021/jm025569k.
(E)-5-(2-Bromovinyl)isodideoxyuridine (BVisoDDU), synthesized on the basis of molecular modeling, is selectively active against HSV-1 (three different strains) but inactive against HSV-2. Unlike BVDU, BVisoDDU is completely resistant to cleavage by thymidine phosphorylase. BVisoDDU is also the first nucleoside analogue lacking OH groups at both the 2'- and 3'-position that shows pronounced activity against HSV-1 replication.
基于分子建模合成的（E）-5-（2-溴乙烯基）异二脱氧尿苷（BVisoDDU）对单纯疱疹病毒1型（三种不同毒株）具有选择性活性，但对单纯疱疹病毒2型无活性。与BVDU不同，BVisoDDU对胸苷磷酸化酶的切割完全耐药。BVisoDDU也是第一种在2'-和3'-位均缺乏羟基但对单纯疱疹病毒1型复制显示出显著活性的核苷类似物。
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