Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease
Journal Article
·
· European Journal of Medicinal Chemistry
- Wichita State Univ., KS (United States)
- Kansas State Univ., Manhattan, KS (United States)
- LiS Consulting, Lawrence, KS (United States)
- Univ. of Kansas, Lawrence, KS (United States)
- Argonne National Lab. (ANL), Argonne, IL (United States)
Norovirus infections have a major impact on public health worldwide, yet there is a current dearth of norovirus-specific therapeutics and prophylactics. Furthermore, 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.
- Research Organization:
- Argonne National Laboratory (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- USDOE Office of Science (SC), Basic Energy Sciences (BES); National Inst. of Health; National Inst. of General Medical Sciences
- Grant/Contract Number:
- AC02-06CH11357; AI109039; P30GM110761
- OSTI ID:
- 1368274
- Alternate ID(s):
- OSTI ID: 1416192
- Journal Information:
- European Journal of Medicinal Chemistry, Vol. 127, Issue C; ISSN 0223-5234
- Publisher:
- ElsevierCopyright Statement
- Country of Publication:
- United States
- Language:
- ENGLISH
Cited by: 8 works
Citation information provided by
Web of Science
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