Novel HCV NS5B polymerase inhibitors derived from 4-(1′,1′-dioxo-1′,4′-dihydro-1′λ6-benzo[1′,2′,4′]thiadiazin-3′-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 20, 2008, Pages 5635-5639

  Dragovich, Peter S ^a   Blazel, Julie K ^a   Ellis, David A ^a   Han, Qing ^a   Kamran, Ruhi ^a   Kissinger, Charles R ^a   LeBrun, Laurie A ^a   Li, Lian Sheng ^a   Murphy, Douglas E ^a   Noble, Michael ^a   Patel, Rupal A ^a   Ruebsam, Frank ^a   Sergeeva, Maria V ^a   Shah, Amit M ^a   Showalter, Richard E ^a   Tran, Chinh V ^a   Tsan, Mei ^a   Webber, Stephen E ^a   Kirkovsky, Leo ^a   Zhou, Yuefen ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

5 Hydroxy 3(2H) pyridazinone derivatives; Hepatitis C virus (HCV); Non nucleoside NS5B inhibitors; Pyridazinones; RNA dependent RNA polymerase (RdRp)

Indexed keywords

4 (1',1' DIOXO 1',4' DIHYDRO 1'LAMBDA6 BENZO[1',2',4']THIADIAZIN 3' YL) 5 HYDROXY 2H PYRIDAZIN 3 ONE DERIVATIVE; ATENOLOL; NONSTRUCTURAL PROTEIN 5B; NS5B PROTEIN POLYMERASE INHIBITOR; PROPRANOLOL; PYRIDAZINONE DERIVATIVE; RNA DEPENDENT RNA POLYMERASE INHIBITOR; RNA DIRECTED RNA POLYMERASE; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; COMPLEX FORMATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG PROTEIN BINDING; HEPATITIS C VIRUS; HUMAN; HUMAN CELL; HUMAN TISSUE; IN VITRO STUDY; LIVER MICROSOME; VIRUS INHIBITION;

ANTIVIRAL AGENTS; CACO-2 CELLS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; CYCLIC S-OXIDES; DNA-DIRECTED RNA POLYMERASES; DRUG DESIGN; GENOTYPE; HUMANS; INHIBITORY CONCENTRATION 50; MICROSOMES; MODELS, CHEMICAL; MOLECULAR CONFORMATION; PYRIDAZINES; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZINES; VIRAL NONSTRUCTURAL PROTEINS;

HEPATITIS C VIRUS;

EID: 53349167272     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.094     Document Type: Article

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39. The O atom at the 5-position of the pyridazinone in Figure 3 was arbitrarily drawn in the protonated form. The precise extent of the protonation was not determined.