Arylethynyltriazole acyclonucleosides inhibit hepatitis C virus replication

  • Bioorg Med Chem Lett. 2008 Jun 1;18(11):3321-7. doi: 10.1016/j.bmcl.2008.04.026.
Ruizhi Zhu  1 ,  Menghua Wang ,  Yi Xia ,  Fanqi Qu ,  Johan Neyts ,  Ling Peng
Affiliations
  • 1. College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430072, PR China.
PMID: 18445526 DOI: 10.1016/j.bmcl.2008.04.026
Abstract

Novel acyclic triazole nucleosides with various ethynyl moieties appended on the triazole nucleobase were synthesized efficiently using a convenient one-step Sonogashira reaction in aqueous solution and under microwave irradiation. One of the compounds, 1f, inhibited HCV subgenomic replication with a 50% effective concentration (EC(50)) of 22 microg/ml and did not inhibit proliferation of the host cell at a concentration of 50 microg/ml. A preliminary SAR study suggests that the appended phenyl ring as well as the rigid triple bond linker contributes importantly to the anti-HCV activity.