Guenther Sven, Balzarini Jan, De Clercq Erik, Nair Vasu
Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602, USA.
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。
