Journal of Medicinal Chemistry p. 290 - 306 (2017)
Update date:2022-08-15
Topics:
Tong, Ling
Yu, Wensheng
Chen, Lei
Selyutin, Oleg
Dwyer, Michael P.
Nair, Anilkumar G.
Mazzola, Robert
Kim, Jae-Hun
Sha, Deyou
Yin, Jingjun
Ruck, Rebecca T.
Davies, Ian W.
Hu, Bin
Zhong, Bin
Hao, Jinglai
Ji, Tao
Zan, Shuai
Liu, Rong
Agrawal, Sony
Xia, Ellen
Curry, Stephanie
McMonagle, Patricia
Bystol, Karin
Lahser, Frederick
Carr, Donna
Rokosz, Laura
Ingravallo, Paul
Chen, Shiying
Feng, Kung-I
Cartwright, Mark
Asante-Appiah, Ernest
Kozlowski, Joseph A.
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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