Synthesis and Antiviral Activity of Novel Methylene Cyclopropyl Nucleosides

  • kwak, Eun-Yee (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University) ;
  • Hong, Joon-Hee (Department of Medicinal Chemistry, College of Pharmacy, Ewha Womans University) ;
  • Lee, Chong-Kyo (Pharmaceutical Screening Center, Korea Research Institute of Chemical Technology) ;
  • Choi, Bo-Gil (Department of Medicinal Chemistry, College of Pharmacy, Chonnam National University)
  • Published : 2000.12.01

Abstract

Novel exomethylene cyclopropyl nucleosides were synthesized as potential antiviral agents. The key intermediate 5 was synthesized in 4 steps, from Feists acid 1 and was condensed with purine derivatives by the $S_N2$ type reaction to give some cyclopropyl nucleosides. The synthesized nucleosides did not showed any significant antiviral activity against HSV-1, HSV-2, HCMV, HIV-1, HIV-2, and HBV up to 100 $\mu\textrm{m}$.

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