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YKZhangPoster125forACS2010SpringMeeting20100321 - Y-K...

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Unformatted text preview: Y.-K. Zhang1, X. Li1, S. Zhang1, Y. Liu1, C. Z. Ding1, Q. Li1, Y.¡Zhou1, J. J. Plattner1, S. J. Baker1, L. Feng1, L. Liu1, W. M. Kazmierski2, M. Duan2, J.-J. Ji2, J. P. Cooper2, R. M. Grimes2, M. D. Tallant2, L. L. Wright2, G. K. Smith2, R. M. Crosby2, A. A. Wang2, R. L. Jarvest3, M. J. Slater3, C. M. Edge3, J. A. Hubbard3, P. Nassau3, B. McDowell3, T. J. Skarzynski3, W. Zou4, X. Dong4, P. Liang4, J. Xiao4, G. Li4, S. Wang4, C. Li4, G. Lü4, B. Zhao4, X. Zhou4, J. Wright4, Z.-J. Ni5, X. Qian5, D. Fan5, L. Liao5, D. Chen5.Poster will be available at www.anacor.com1Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA; 2GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC;3GlaxoSmithKline, Gunnels Wood Road, Stevenage, Herts, UK; 4BioDuro LLC, Life Science Park Road, Changping District, Beijing, China; 5Acme Bioscience, Inc., 3941 E. Bayshore Road, Palo Alto, CA.Macrocyclic HCV NS3/4A Serine Protease Inhibitors with Benzoxaborole at P4 Position: Design, Synthesis and SAR MEDI 125of 239thACS National Meeting, San Francisco, March 21, 2010AbstractIn an ongoing HCV protease inhibition program, one of the strategies we used for our design of proprietary HCV protease inhibitors is to link a stable and novel boron-containing moiety, benzoxaborole (CBO), to a known HCV protease inhibitory macrocyclic template at P4 position. We have synthesized three series of CBO-containing inhibitors with different P2* groups. We investigated the impact of CBO ring orientation and substitutions, the linking group in between CBO ring and macrocycle on series (a) with isoindoline P2*....
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