Hiroshi Hosono

Synthesis of Thymidine Derivatives 3′-Modified with a Polar Three-Atom Group as Potential Anti-HIV-1 Agents

Abstract 3′-Modified thymidine analogs, such as 3′-O-[(methylthio)thio-carbonyl]thymidine (4), 3′-O-thiocarbamoylthymidine (7), and N-(3′-deoxy-thymidin-3′-y1)phosphoramidates (9a, b), were synthesized from thymidine derivatives (1), (5), and (8), respectively, as potential anti-human immunodeficiency virus type 1 (HIV-1) agents. No significant activity against HIV-1 was, however, observed with any of these compounds.