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The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase

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Abstract

The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented. Many challenges, including poor oral bioavailability, high clearance, bioactivation, high human serum shift, and metabolic stability were encountered and overcome through SAR studies. This work culminated in the selection of BMS-986139 (43) as a preclinical candidate.

Graphical abstract: The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase

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Publication details

The article was received on 15 Nov 2016, accepted on 20 Jan 2017, published on 08 Feb 2017 and first published online on 08 Feb 2017


Article type: Research Article
DOI: 10.1039/C6MD00636A
Citation: Med. Chem. Commun., 2017, Advance Article
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    The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase

    K. J. Eastman, K. Parcella, K. Yeung, K. A. Grant-Young, J. Zhu, T. Wang, Z. Zhang, Z. Yin, B. R. Beno, S. Sheriff, K. Kish, J. Tredup, A. G. Jardel, V. Halan, K. Ghosh, D. Parker, K. Mosure, H. Fang, Y. Wang, J. Lemm, X. Zhuo, U. Hanumegowda, K. Rigat, M. Donoso, M. Tuttle, T. Zvyaga, Z. Haarhoff, N. A. Meanwell, M. G. Soars, S. B. Roberts and J. F. Kadow, Med. Chem. Commun., 2017, Advance Article , DOI: 10.1039/C6MD00636A

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