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Volumn 18, Issue 16, 2008, Pages 4628-4632

4-(1,1-Dioxo-1,4-dihydro-1λ6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase

Author keywords

4 (1,1 Dioxo 1,4 dihydro 1 6 benzo 1,4 thiazin 3 yl) 5 hydroxy 2H pyridazin 3 one; Hepatitis C virus (HCV); Non nucleoside NS5B inhibitor; NS5B polymerase; Structure based design

Indexed keywords

BENZOTHIAZINE DERIVATIVE; ENZYME INHIBITOR; NONSTRUCTURAL PROTEIN 5B; PYRIDAZINONE DERIVATIVE; VIRUS ENZYME;

EID: 48649092953     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.07.014     Document Type: Article
Times cited : (29)

References (27)
  • 14
    • 48649086445 scopus 로고    scopus 로고
    • Blake, J. F.; Fell, J. B.; Fischer, J. P.; Hendricks, R. T.; Spencer, S. R.; Stengel, P. J. WO2006117306, 2006
    • Blake, J. F.; Fell, J. B.; Fischer, J. P.; Hendricks, R. T.; Spencer, S. R.; Stengel, P. J. WO2006117306, 2006
  • 16
    • 48649108709 scopus 로고    scopus 로고
    • Hutchinson, D. K. et al. U.S. Patent US2005107364, 2005
    • Hutchinson, D. K. et al. U.S. Patent US2005107364, 2005
  • 18
    • 48649108863 scopus 로고    scopus 로고
    • All structures are arbitrarily drawn as one of several possible tautomers.
    • All structures are arbitrarily drawn as one of several possible tautomers.
  • 25
    • 48649090847 scopus 로고    scopus 로고
    • Related benzothiazine-containing NS5B inhibitors have been reported by others as well. Intermediates 7, 8, 10, 11, and 12 were prepared as described in: Blake, F. J. et al. U.S. Patent Application US20060040972, 2006.
    • Related benzothiazine-containing NS5B inhibitors have been reported by others as well. Intermediates 7, 8, 10, 11, and 12 were prepared as described in: Blake, F. J. et al. U.S. Patent Application US20060040972, 2006.
  • 26
    • 48649085246 scopus 로고    scopus 로고
    • 2 at pH 7.6, and an inhibitor concentration of 2-10 mM. Diffraction data were collected to a resolution of 2.1 Å for compound 3a. The crystal structure discussed in this Letter has been deposited in the Protein Databank (http://www.rcsb.org) with entry code: 3CWJ. Full structure determination details are given in the PDB entry.
    • 2 at pH 7.6, and an inhibitor concentration of 2-10 mM. Diffraction data were collected to a resolution of 2.1 Å for compound 3a. The crystal structure discussed in this Letter has been deposited in the Protein Databank (http://www.rcsb.org) with entry code: 3CWJ. Full structure determination details are given in the PDB entry.
  • 27
    • 48649107871 scopus 로고    scopus 로고
    • The reduced stability of 5b toward monkey liver microsomes relative to 5a may also have contributed to the lower bioavailability of the former compound.
    • The reduced stability of 5b toward monkey liver microsomes relative to 5a may also have contributed to the lower bioavailability of the former compound.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.