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Synthesis and evaluation of novel a-amino cyclic boronates as inhibitors of HCV NS3 protease
journal contribution
posted on 2023-06-08, 21:48 authored by Xianfeng Li, Yong-Kang Zhang, Yang Liu, Charles Z Ding, Qun Li, Yasheen Zhou, Jacob J Plattner, Stephen J Baker, Xuelei Qian, Dazhong Fan, Liang Liao, Zhi-Jie Ni, Gemma V White, Jackie E Mordaunt, Linos X Lazarides, Martin J Slater, Richard L Jarvest, Pia Thommes, Malcolm Ellis, Colin M Edge, Julia A Hubbard, Don Somers, Paul Rowland, Pamela Nassau, Bill McDowell, Tadeusz J Skarzynski, Wieslaw M Kazmierski, Richard M Grimes, Lois L. Wright, Gary K Smith, Wuxin Zou, Jon Wright, Lewis E PennicottWe have designed and synthesized a novel series of alpha-amino cyclic boronates and incorporated them successfully in several acyclic templates at the P1 position. These compounds are inhibitors of the HCV NS3 serine protease, and structural studies show that they inhibit the NS3 protease by trapping the Ser-139 hydroxyl group in the active site. Synthetic methodologies and SARs of this series of compounds are described.
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Publication status
- Published
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- Published version
Journal
Bioorganic and Medicinal Chemistry LettersISSN
0960-894XPublisher
ElsevierExternal DOI
Issue
12Volume
20Page range
3550-3556Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2015-07-21First Compliant Deposit (FCD) Date
2015-07-20Usage metrics
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