MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV

  • Bioorg Med Chem Lett. 2018 Jun 1;28(10):1954-1957. doi: 10.1016/j.bmcl.2018.03.049.
Anilkumar G Nair  1 ,  Qingbei Zeng  2 ,  Oleg Selyutin  2 ,  Stuart B Rosenblum  2 ,  Yueheng Jiang  2 ,  De-Yi Yang  2 ,  Kerry Keertikar  2 ,  Guowei Zhou  2 ,  Michael Dwyer  2 ,  Seong Heon Kim  2 ,  Bandarpalle Shankar  2 ,  Wensheng Yu  2 ,  Ling Tong  2 ,  Lei Chen  2 ,  Robert Mazzola  2 ,  John Caldwell  2 ,  Haiqun Tang  2 ,  Sony Agrawal  2 ,  Rong Liu  2 ,  Rong Kong  2 ,  Paul Ingravallo  2 ,  Ellen Xia  2 ,  Ying Zhai  2 ,  Amin Nomeir  2 ,  Ernest Asante-Appiah  2 ,  Joseph A Kozlowski  2
Affiliations
  • 1. Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: [email protected].
  • 2. Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
PMID: 29653894 DOI: 10.1016/j.bmcl.2018.03.049
Abstract

HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral fixed dose combination regimen. Herein, we describe the discovery and characterization of silyl proline-containing HCV NS5A inhibitor MK-8325 with good pan-genotype activity and acceptable pharmacokinetic properties.

Keywords
Antiviral; HCV; NS5A; Silyl proline.
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