Synthesis and anti-HIV activity of C4-modified pyrimidine nucleosides

Abstract

One-pot syntheses provided a series of triazole- and pentafluorophenyloxy-substituted pyrimidine nucleosides. Most of the compounds in the series displayed anti-HIV activities but none as potent as AZT 2. 1-(β- d- Erythro-pentofuranosyl)-4-pentafluorophenyloxy-2(1 H)-pyrimidinone 14 was the most potent and the most selective compound in the series with EC 50=1.6 μM.