Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease

Vishnu C. Damalanka, Yunjeong Kim, Anushka C. Galasiti Kankanamalage, Gerald H. Lushington, Nurjahan Mehzabeen, Kevin P. Battaile, Scott Lovell, Kyeong Ok Chang, William C. Groutas

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

Norovirus infections have a major impact on public health worldwide, yet there is a current dearth of norovirus-specific therapeutics and prophylactics. This report describes the discovery of a novel class of macrocyclic inhibitors of norovirus 3C-like protease, a cysteine protease that is essential for virus replication. SAR, structural, and biochemical studies were carried out to ascertain the effect of structure on pharmacological activity and permeability. Insights gained from these studies have laid a solid foundation for capitalizing on the therapeutic potential of the series of inhibitors described herein.

Original languageEnglish
Pages (from-to)41-61
Number of pages21
JournalEuropean Journal of Medicinal Chemistry
Volume127
DOIs
StatePublished - 2017

Keywords

  • 3CLprotease
  • Macrocyclic inhibitors
  • Norovirus

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