Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7317-7322

  Ding, Charles Z ^a   Zhang, Yong Kang ^a   Li, Xianfeng ^a   Liu, Yang ^a   Zhang, Suoming ^a   Zhou, Yasheen ^a   Plattner, Jacob J ^a   Baker, Stephen J ^a   Liu, Liang ^a   Duan, Maosheng ^b   Jarvest, Richard L ^c   Ji, Jingjing ^b   Kazmierski, Wieslaw M ^b   Tallant, Matthew D ^b   Wright, Lois L ^b   Smith, Gary K ^b   Crosby, Renae M ^b   Wang, Amy A ^b   Ni, Zhi Jie ^d   Zou, Wuxin ^e   Wright, Jon ^e   more..

^a PFIZER INC   (United States)

^b GLAXOSMITHKLINE   (United States)

^c GLAXOSMITHKLINE   (United Kingdom)

^d Acme Bioscience Inc   (United States)

^e BioDuro LLC   (China)

Author keywords

Benzoxaborole; HCV; HCV NS3 protease inhibitors; HCV protease inhibitors; Synthesis and biological evaluations

Indexed keywords

BENZOXABOROLE; BMS 791325; ISOQUINOLINE; ITMN 191; MACROCYCLIC COMPOUND; NONSTRUCTURAL PROTEIN 3; ORGANOBORON DERIVATIVE; PROTEINASE INHIBITOR; THIAZOLE; TMC 435350; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; HEPATITIS C VIRUS; NONHUMAN; RAT; REPLICON; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTIVIRAL AGENTS; HEPACIVIRUS; ISOQUINOLINES; MACROCYCLIC COMPOUNDS; PROTEASE INHIBITORS; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; VIRAL NONSTRUCTURAL PROTEINS;

HEPATITIS C VIRUS;

EID: 78449289368     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.071     Document Type: Article

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33. (a) Preliminary results of co-crystal structure of compound 4 with HCV protease enzyme did not show specific ligand-protein interactions. Co-crystal structures with other ligands were unknown; (b) Publication of the series is pending.