Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 23, 2012, Pages 7207-7213

  Rudd, Michael T ^a   McIntyre, Charles J ^a   Romano, Joseph J ^a   Butcher, John W ^a   Holloway, M Katharine ^a   Bush, Kimberly ^a   Nguyen, Kevin T ^a   Gilbert, Kevin F ^a   Lyle, Terry A ^a   Liverton, Nigel J ^a   Wan, Bang Lin ^a   Summa, Vincenzo ^b   Harper, Steven ^b   Rowley, Michael ^b   Vacca, Joseph P ^a   Carroll, Steven S ^a   Burlein, Christine ^a   Dimuzio, Jillian M ^a   Gates, Adam ^a   Graham, Donald J ^a   Huang, Qian ^a   Ludmerer, Steven W ^a   McClain, Stephanie ^a   McHale, Carolyn ^a   Stahlhut, Mark ^a   Fandozzi, Christine ^a   Taylor, Anne ^a   Trainor, Nicole ^a   Olsen, David B ^a   McCauley, John A ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b IRBM   (Italy)

Author keywords

Cyclic constraint; Hepatitis C; Macrocycle; NS3 4A protease; P2 P4 linker

Indexed keywords

HEPATITIS C NS3 PROTEASE; MACROCYCLIC COMPOUND; MUTANT PROTEIN; PROTEINASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG CONFORMATION; DRUG POTENCY; DRUG STRUCTURE; GENOTYPE; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VIRUS REPLICATION;

ANIMALS; BINDING SITES; CARRIER PROTEINS; CATALYTIC DOMAIN; CYCLIZATION; GENOTYPE; HALF-LIFE; HEPACIVIRUS; KINETICS; LIVER; MACROCYCLIC COMPOUNDS; MOLECULAR DOCKING SIMULATION; MUTATION; PROTEASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; VIRAL NONSTRUCTURAL PROTEINS;

HEPATITIS C VIRUS; RATTUS;

EID: 84869083921     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.09.061     Document Type: Article

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