SYNTHESIS AND ANTI-HERPES VIRUS ACTIVITY OF 2'-DEOXY-4'-THIOPYRIMIDINE NUCLEOSIDES

A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was s ynthesized and evaluated as potential antiviral agents. A number of an alogues such as 2'-deoxy-5-propyl-4'-thiouridine (3ii), 2'-deoxy-5-iso propyl-4'-thiouridine (3iii), 5-cyclopropyl-2'-deoxy-4'-thiouridine (3 iv), 2'-deoxy-4'-thio-5-vinyluridine (3viii), and 5-(2-chloroethyl)-2' -deoxy-4'-thiouridin (3xx) were found to be highly active against herp es simplex virus type-1 (HSV-1) and varicella tester virus (VZV) in vi tro with no significant cytotoxicity. The compound with the broadest s pectrum of activity was 2'-deoxy-5-ethyl-4'-thiouridine (3i) which sho wed significant activity against HSV-1, HSV-2, and VZV.