Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: Exploration of P2 quinazoline substituents

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 14, 2010, Pages 4004-4011

  Nilsson, Magnus ^a   Belfrage, Anna Karin ^a,c   Lindström, Stefan ^a   Wähling, Horst ^a   Lindquist, Charlotta ^a   Ayesa, Susana ^a   Kahnberg, Pia ^a   Pelcman, Mikael ^a   Benkestock, Kurt ^a   Agback, Tatiana ^a   Vrang, Lotta ^a   Terelius, Ylva ^a   Wikström, Kristina ^a   Hamelink, Elizabeth ^a   Rydergård, Christina ^a   Edlund, Michael ^a   Eneroth, Anders ^a   Raboisson, Pierre ^b   Lin, Tse I ^b   de Kock, Herman ^b   Wigerinck, Piet ^b   Simmen, Kenneth ^b   Samuelsson, Bertil ^a   Rosenquist, Åsa ^a   more..

^a MEDIVIR AB   (Sweden)

^b JANSSEN RESEARCH FOUNDATION   (Belgium)

^c UPPSALA UNIVERSITY   (Sweden)

Author keywords

DMPK; HCV; In vitro; In vivo PK; Inhibitors; NS3 4A protease; P2 substituent; Quinazoline; Replicon assay

Indexed keywords

ANTIVIRUS AGENT; CYCLOPENTANE DERIVATIVE; DICARBOXYLIC ACID DERIVATIVE; MACROCYCLIC COMPOUND; NONSTRUCTURAL PROTEIN 3; NONSTRUCTURAL PROTEIN 4A; PROLINE DERIVATIVE; PROTEINASE INHIBITOR; QUINAZOLINE DERIVATIVE; UREA DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; CELL MEMBRANE PERMEABILITY; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EXPOSURE; DRUG LIVER LEVEL; DRUG POTENCY; DRUG STABILITY; DRUG SYNTHESIS; HEPATITIS C VIRUS; HUMAN; HUMAN CELL; IN VIVO STUDY; LIVER MICROSOME; MALE; NONHUMAN; RAT; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

AREA UNDER CURVE; CACO-2 CELLS; CARRIER PROTEINS; HEPACIVIRUS; HUMANS; MICROSOMES, LIVER; PROTEASE INHIBITORS; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; VIRAL NONSTRUCTURAL PROTEINS; VIRAL PROTEINS;

HEPATITIS C VIRUS; RATTUS;

EID: 77953873770     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.05.029     Document Type: Article

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