Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease

Li, Xianfeng, Zhang, Yong-Kang, Liu, Yang, Ding, Charles Z, Li, Qun, Zhou, Yasheen, Plattner, Jacob J, Baker, Stephen J, Qian, Xuelei, Fan, Dazhong, Liao, Liang, Ni, Zhi-Jie, White, Gemma V, Mordaunt, Jackie E, Lazarides, Linos X, Slater, Martin J, Jarvest, Richard L, Thommes, Pia, Ellis, Malcolm, Edge, Colin M, Hubbard, Julia A, Somers, Don, Rowland, Paul, Nassau, Pamela, McDowell, Bill, Skarzynski, Tadeusz J, Kazmierski, Wieslaw M, Grimes, Richard M, Wright, Lois L., Smith, Gary K, Zou, Wuxin, Wright, Jon and Pennicott, Lewis E (2010) Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease. Bioorganic and Medicinal Chemistry Letters, 20 (12). pp. 3550-3556. ISSN 0960-894X

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Abstract

We 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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry > QD0241 Organic chemistry
Depositing User: Lewis Pennicott
Date Deposited: 21 Jul 2015 06:57
Last Modified: 08 Mar 2017 06:42
URI: http://sro.sussex.ac.uk/id/eprint/55652

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