Article
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.
Bioorganic & medicinal chemistry letters - 1 Dec 2012
Rudd Michael T, McCauley John A, Romano Joseph J, Butcher John W, Bush Kimberly, McIntyre Charles J, Nguyen Kevin T, Gilbert Kevin F, Lyle Terry A, Holloway M Katharine, Wan Bang-Lin, Vacca Joseph P, Summa Vincenzo, Harper Steven, Rowley Michael, Carroll Steven S, Burlein Christine, DiMuzio Jillian M, Gates Adam, Graham Donald J, Huang Qian, Ludmerer Steven W, McClain Stephanie, McHale Carolyn, Stahlhut Mark, Fandozzi Christine, Taylor Anne, Trainor Nicole, Olsen David B, Liverton Nigel J
Abstract excerpt
A series of macrocyclic compounds containing 2-substituted-quinoline moieties have been discovered and shown to exhibit excellent HCV NS3/4a genotype 3a and genotype 1b R155K mutant activity while maintaining the high rat liver exposure. Cyclization of the 2-substituted quinoline substituent led to a series of tricyclic P2 compounds which also display superb gt3a potency.
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