A thymidine phosphorylase-stable analogue of BVDU with significant antiviral activity

被引：19

作者：

Guenther, S

Balzarini, J

De Clercq, E

Nair, V ^{[1
]}

机构：

[1] Univ Georgia, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA

[2] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA

[3] Rega Inst, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 25期

关键词：

D O I：

10.1021/jm025569k

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(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.

引用

页码：5426 / 5429

页数：4

共 12 条

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2-8

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