Novel antiviral activity of l-dideoxy bicyclic nucleoside analogues versus vaccinia and measles viruses in vitro

J Med Chem. 2013 Feb 14;56(3):1311-22. doi: 10.1021/jm301778x. Epub 2013 Jan 29.

Abstract

Dideoxy bicyclic pyrimidine nucleoside analogues (ddBCNAs) with d-chirality have previously been described by us to inhibit replication of human cytomegalovirus. We herein report for the first time that activity against vaccinia virus (VACV) was achieved using novel l-analogues. A structure-activity relationship was established: Antiviral activity versus VACV was highest with an ether side chain with an optimum of n-C(9)H(18)-O-n-C(5)H(11). This gave an IC(50) of 190 nM, a 60-fold enhancement over the FDA-approved antiviral cidofovir. Interestingly, l-ddBCNAs also inhibit wild type measles virus syncytia formation with a TCID(50) of 7.5 μM for the lead compound. We propose that l-ddBCNAs represent significant innovative antiviral candidates versus measles and poxviruses, and we suggest a mechanism of action versus one or more cellular targets that are essential for viral replication.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • HeLa Cells
  • Humans
  • In Vitro Techniques
  • Magnetic Resonance Spectroscopy
  • Measles virus / drug effects*
  • Measles virus / growth & development
  • Microbial Sensitivity Tests
  • Spectrometry, Mass, Electrospray Ionization
  • Vaccinia virus / drug effects*
  • Vaccinia virus / growth & development
  • Viral Plaque Assay

Substances

  • Antiviral Agents