2. Academic Validation
  3. Potent bisimidazole-based HCV NS5A inhibitors bearing annulated tricyclic motifs

Potent bisimidazole-based HCV NS5A inhibitors bearing annulated tricyclic motifs

  • Bioorg Med Chem Lett. 2014 Dec 15;24(24):5738-5742. doi: 10.1016/j.bmcl.2014.10.056.
Min Zhong 1,  Eric Peng 2,  Ningwu Huang 2,  Qi Huang 2,  Anja Huq 2,  Meiyen Lau 2,  Richard Colonno 2,  Leping Li 3
Affiliations

Affiliations

  • 1 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: min.zhong@acmeca.com.
  • 2 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA.
  • 3 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: lli@presidiopharma.com.
PMID: 25453811 DOI: 10.1016/j.bmcl.2014.10.056
Abstract

This Letter describes the synthesis and biological evaluation of a number of functionalized bisimidazoles bearing annulated tricyclic motifs as potent inhibitors of HCV NS5A protein. Compound 4 h, which contains a substituted tricyclic 6-6-6 xanthene, demonstrated broad genotypic spectrum, compelling potency, and good oral bioavailability with dose-dependent drug exposure level in multiple animal species.

Keywords

Annulated tricyclic; Bisimidazole; HCV; NS5A inhibitor.

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