Emimycin and its nucleoside derivatives: Synthesis and antiviral activity

  • Eur J Med Chem. 2018 Jan 20:144:93-103. doi: 10.1016/j.ejmech.2017.12.018.
Elzbieta Plebanek  1 ,  Eveline Lescrinier  1 ,  Graciela Andrei  2 ,  Robert Snoeck  2 ,  Piet Herdewijn  1 ,  Steven De Jonghe  3
Affiliations
  • 1. Medicinal Chemistry, Rega Institute for Medical Research, KU Leuven, Herestraat 49 - bus 1041, 3000 Leuven, Belgium.
  • 2. Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Herestraat 49 - bus 1043, 3000 Leuven, Belgium.
  • 3. Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Herestraat 49 - bus 1043, 3000 Leuven, Belgium. Electronic address: [email protected].
PMID: 29268134 DOI: 10.1016/j.ejmech.2017.12.018
Abstract

The synthesis of emimycin, 5-substituted emimycin analogues and the corresponding ribo- and 2'-deoxyribonucleoside derivatives is described. Emimycin, its 5-substituted congeners and the ribonucleoside derivatives are completely devoid of Antiviral activity against RNA viruses. In contrast, some of the 2'-deoxyribosyl emimycin derivatives are potent inhibitors of the replication of herpes simplex virus-1 and varicella-zoster virus, lacking cytotoxicity.

Keywords
Antiviral; Emimycin; Nucleoside; Pyrazine.
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