Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms | Zendy

Ling Tong | Zendy; Wensheng Yu | Zendy; Lei Chen | Zendy; Oleg Selyutin | Zendy; Michael P. Dwyer | Zendy; Anilkumar G. Nair | Zendy; Robert Mazzola | Zendy; JaeHun Kim | Zendy; Deyou Sha | Zendy; Jingjun Yin | Zendy; Rebecca T. Ruck | Zendy; Ian W. Davies | Zendy; Bin Hu | Zendy; Bin Zhong | Zendy; Jinglai Hao | Zendy; Tao Ji | Zendy; Shuai Zan | Zendy; Rong Liu | Zendy; Sony Agrawal | Zendy; Ellen Xia | Zendy; Stephanie Curry | Zendy; Patricia McMonagle | Zendy; Karin Bystol | Zendy; Frederick Lahser | Zendy; Donna Carr | Zendy; Laura L. Rokosz | Zendy; Paul Ingravallo | Zendy; Shiying Chen | Zendy; KungI Feng | Zendy; Mark E. Cartwright | Zendy; Ernest AsanteAppiah | Zendy; Joseph A. Kozlowski | Zendy

Open Access

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms

Author(s) -

Ling Tong,

Wensheng Yu,

Lei Chen,

Oleg Selyutin,

Michael P. Dwyer,

Anilkumar G. Nair,

Robert Mazzola,

JaeHun Kim,

Deyou Sha,

Jingjun Yin,

Rebecca T. Ruck,

Ian W. Davies,

Bin Hu,

Bin Zhong,

Jinglai Hao,

Tao Ji,

Shuai Zan,

Rong Liu,

Sony Agrawal,

Ellen Xia,

Stephanie Curry,

Patricia McMonagle,

Karin Bystol,

Frederick Lahser,

Donna Carr,

Laura L. Rokosz,

Paul Ingravallo,

Shiying Chen,

KungI Feng,

Mark E. Cartwright,

Ernest AsanteAppiah,

Joseph A. Kozlowski

Publication year - 2016

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/acs.jmedchem.6b01310

Subject(s) - ns5a , chemistry , valine , genotype , imidazole , indole test , mutant , virology , pharmacology , hepacivirus , stereochemistry , biochemistry , biology , amino acid , gene

We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A inhibitor contains a unique tetracyclic indole core while maintaining the imidazole-proline-valine Moc motifs of our previous NS5A inhibitors. Compound 40 is currently in early clinical trials and is under evaluation as part of an all-oral DAA regimen for the treatment of chronic HCV infection.

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