| Literature DB >> 27808515 |
Ling Tong, Wensheng Yu, Lei Chen, Oleg Selyutin, Michael P Dwyer, Anilkumar G Nair, Robert Mazzola, Jae-Hun Kim, Deyou Sha, Jingjun Yin, Rebecca T Ruck, Ian W Davies, Bin Hu1, Bin Zhong1, Jinglai Hao1, Tao Ji1, Shuai Zan1, Rong Liu, Sony Agrawal, Ellen Xia, Stephanie Curry, Patricia McMonagle, Karin Bystol, Frederick Lahser, Donna Carr, Laura Rokosz, Paul Ingravallo, Shiying Chen, Kung-I Feng, Mark Cartwright, Ernest Asante-Appiah, Joseph A Kozlowski.
Abstract
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.Entities:
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Year: 2016 PMID： 27808515 DOI： 10.1021/acs.jmedchem.6b01310
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446