1. Academic Validation
  2. Synthesis and characterization of 2'-C-Me branched C-nucleosides as HCV polymerase inhibitors

Synthesis and characterization of 2'-C-Me branched C-nucleosides as HCV polymerase inhibitors

  • Bioorg Med Chem Lett. 2012 Jun 15;22(12):4127-32. doi: 10.1016/j.bmcl.2012.04.065.
Aesop Cho 1 Lijun Zhang Jie Xu Darius Babusis Thomas Butler Rick Lee Oliver L Saunders Ting Wang Jay Parrish Jason Perry Joy Y Feng Adrian S Ray Choung U Kim
Affiliations

Affiliation

  • 1 Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94044, USA. acho@gilead.com
Abstract

A series of 2'-C-methyl branched purine and pyrimidine C-nucleosides were prepared. Their anti-HCV activity and pharmacological properties were profiled, and compared with known 2'-C-Me N-nucleoside counterparts. In particular, 2'-C-Me 4-aza-7,9-dideazaadenosine C-nucleoside (2) was found to have potent and selective anti-HCV activity in vitro as well as a favorable pharmacokinetic profile and in vivo potential for enhanced potency over the corresponding N-nucleoside.

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