Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides

被引:96
|
作者
Rahim, SG [1 ]
Trivedi, N [1 ]
BogunovicBatchelor, MV [1 ]
Hardy, GW [1 ]
Mills, G [1 ]
Selway, JWT [1 ]
Snowden, W [1 ]
Littler, E [1 ]
Coe, PL [1 ]
Basnak, I [1 ]
Whale, RF [1 ]
Walker, RT [1 ]
机构
[1] UNIV BIRMINGHAM,SCH CHEM,BIRMINGHAM B15 2TT,W MIDLANDS,ENGLAND
关键词
D O I
10.1021/jm950029r
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was synthesized and evaluated as potential antiviral agents. A number of analogues such as 2'-deoxy-5-propyl-4'-thiouridine (3ii), 2'-deoxy-5-isopropyl-4'-thiouridine (3iii), 5-cyclopropyl-2'-deoxy-4'-thiouridine (3iv), 2'-deoxy-4'-thio-5-vinyluridine (3viii), and 5-(2-chloroethyl)-2'-deoxy-4'-thiouridin (3xx) were found to be highly active against herpes simplex virus type-1 (HSV-1) and varicella tester virus (VZV) in vitro with no significant cytotoxicity. The compound with the broadest spectrum of activity was 2'-deoxy-5-ethyl-4'-thiouridine (3i) which showed significant activity against HSV-1, HSV-2, and VZV.
引用
收藏
页码:789 / 795
页数:7
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