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

…, Y Zhou, JJ Plattner, SJ Baker, X Qian, D Fan…

文献索引：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; Pennicott, Lewis E. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3550 - 3556

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被引用次数: 25

摘要

We have designed and synthesized a novel series of α-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.