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  • Title: Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides.
    Author: Rahim SG, Trivedi N, Bogunovic-Batchelor MV, Hardy GW, Mills G, Selway JW, Snowden W, Littler E, Coe PL, Basnak I, Whale RF, Walker RT.
    Journal: J Med Chem; 1996 Feb 02; 39(3):789-95. PubMed ID: 8576922.
    Abstract:
    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'-thiouridine (3xx) were found to be highly active against herpes simplex virus type-1 (HSV-1) and varicella zoster 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.
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