Article
P2-quinazolinones and bis-macrocycles as new templates for next-generation hepatitis C virus NS3/4a protease inhibitors: discovery of MK-2748 and MK-6325.
ChemMedChem - 1 Apr 2015
Rudd Michael T, Butcher John W, Nguyen Kevin T, McIntyre Charles J, Romano Joseph J, Gilbert Kevin F, Bush Kimberly J, Liverton Nigel J, Holloway M Katharine, Harper Steven, Ferrara Marco, DiFilippo Marcello, Summa Vincenzo, Swestock John, Fritzen Jeff, Carroll Steven S, Burlein Christine, DiMuzio Jillian M, Gates Adam, Graham Donald J, Huang Qian, McClain Stephanie, McHale Carolyn, Stahlhut Mark W, Black Stuart, Chase Robert, Soriano Aileen, Fandozzi Christine M, Taylor Anne, Trainor Nicole, Olsen David B, Coleman Paul J, Ludmerer Steven W, McCauley John A
Abstract excerpt
With the goal of identifying inhibitors of hepatitis C virus (HCV) NS3/4a protease that are potent against a wide range of genotypes and clinically relevant mutant viruses, several subseries of macrocycles were investigated based on observations made during the discovery of MK-5172. Quinazolinone-containing macrocycles were identified as promising leads, and optimization for superior cross-genotype and mutant...
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