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

Pennicott, Lewis (2010) Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease. Bioorganic & Medicinal Chemistry Letters, 20 (12). pp. 3550-3556. ISSN 0960894X

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Abstract

We have designed and synthesized a novel series of -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
Additional Information: (with Xianfeng Lia, 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, and Jon Wright)
Schools and Departments: School of Life Sciences > Chemistry
Depositing User: Lewis Pennicott
Date Deposited: 06 Feb 2012 18:19
Last Modified: 31 May 2012 13:58
URI: http://sro.sussex.ac.uk/id/eprint/15750
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