Synthesis and antiviral evaluation of 3′-substituted thymidine analogues derived from 3′-amino-3′-deoxythymidine

Article abstract of DOI:10.1016/0040-4020(95)00198-H

Based on the structure-activity relationship for antiviral activity, a series of 3′-deoxy-3′-N-functionalized thymidine analogues derived from 3′-amino-3′-deoxythymidine was synthesized. These compounds were evaluated for their antiviral activity. Three of the prepared molecules namely 3′-(1,2,4-triazol-1-yl)carbimidoylamino-3′-deoxythymidine 6, 3′-(3-amino-1-methyl-1,2,4-triazol-5-yl)amino-3′-deoxythymidine 8b and 3′-N-cyano-O-phenylisourea-3′-deoxythymidine 7 show moderate but selective in vitro activity against HIV-1 and HIV-2. These data demonstrate that some steric bulk in the 3′-position is compatible with anti-HIV activity. Copyright