Article
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.
Journal of medicinal chemistry - 23 Apr 2020
Kazmierski Wieslaw M, Baskaran Sam, Walker Jill T, Miriyala Nagaraju, Meesala Ramu, Beesu Mallesh, Adjabeng George, Grimes Richard M, Hamatake Robert, Leivers Martin R, Crosby Renae, Xia Bing, Remlinger Katja
Abstract excerpt
Pan-genotype NS5A inhibitors underpin hugely successful hepatitis C virus (HCV) therapy. The discovery of GSK2818713 (13), a nonstructural protein 5A (NS5A) HCV inhibitor characterized by a significantly improved genotype coverage relative to first-generation NS5A inhibitor daclatasvir (DCV), is detailed herein. The SAR analysis revealed cooperative potency effects of the biphenylene, bicyclic pyrrolidine (Aoc),...
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