期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 127, 期 -, 页码 41-61出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.12.033
关键词
Macrocyclic inhibitors; Norovirus; 3CLprotease
资金
- National Institutes of Health [AI109039]
- National Institute of General Medical Sciences [P30GM110761]
- National Institutes of Health
- companies of the Industrial Macromolecular Crystallography Association through Hauptman Woodward Medical Research Institute
- U.S. Department of Energy, Office of Science, Office of Basic Energy Sciences [DE-ACO2-06CH11357]
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. (C) 2016 Elsevier Masson SAS. All rights reserved.
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