메뉴 건너뛰기




Volumn 5, Issue 3, 2014, Pages 240-243

Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors

Author keywords

HCV; NS5A; Thienoimidazoles

Indexed keywords

ACETYLENE DERIVATIVE; ANTIVIRUS AGENT; BENZIMIDAZOLE; BORONIC ACID DERIVATIVE; IMIDAZOLE DERIVATIVE; NONSTRUCTURAL PROTEIN 5A INHIBITOR;

EID: 84990931466     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml300461f     Document Type: Article
Times cited : (16)

References (20)
  • 1
    • 79958717571 scopus 로고    scopus 로고
    • The global health burden of hepatitis C virus infection
    • Negro, F.; Alberti, A. The global health burden of hepatitis C virus infection. Liver Int. 2011, 31, 1-3.
    • (2011) Liver Int. , vol.31 , pp. 1-3
    • Negro, F.1    Alberti, A.2
  • 2
    • 23944482649 scopus 로고    scopus 로고
    • Challenges and successes in developing new therapies for hepatitis C
    • For reviews, see De Francesco, R.; Migliaccio, G. Challenges and successes in developing new therapies for hepatitis C. Nature 2005, 436, 953.
    • (2005) Nature , vol.436 , pp. 953
    • De Francesco, R.1    Migliaccio, G.2
  • 3
    • 23944452579 scopus 로고    scopus 로고
    • Prospect for a vaccine against the hepatitis C virus
    • Houghton, M.; Abrignani, S. Prospect for a vaccine against the hepatitis C virus. Nature 2005, 436, 961-966.
    • (2005) Nature , vol.436 , pp. 961-966
    • Houghton, M.1    Abrignani, S.2
  • 4
    • 23944462641 scopus 로고    scopus 로고
    • Mechanism of action of interferon and ribavirin in treatment of hepatitis C
    • Feld, J. J.; Hoofnagle, J. H. Mechanism of action of interferon and ribavirin in treatment of hepatitis C. Nature 2005, 436, 967-972.
    • (2005) Nature , vol.436 , pp. 967-972
    • Feld, J.J.1    Hoofnagle, J.H.2
  • 5
    • 84865291164 scopus 로고    scopus 로고
    • Protease inhibitors for the treatment of chronic hepatitis C genotype-1 infection: The new standard of care
    • Pearlman, B. L. Protease inhibitors for the treatment of chronic hepatitis C genotype-1 infection: the new standard of care. Lancet Inf. Dis. 2012, 12, 717-728.
    • (2012) Lancet Inf. Dis. , vol.12 , pp. 717-728
    • Pearlman, B.L.1
  • 6
    • 79952170631 scopus 로고    scopus 로고
    • Hepatitis C virus NS3/4A proteases inhibitors: A light at the end of the tunnel
    • Chatel-Chaix, L.; Baril, M.; Lamarre, D. Hepatitis C Virus NS3/4A Proteases Inhibitors: A Light at the End of the Tunnel. Viruses 2010, 2, 1752-1765.
    • (2010) Viruses , vol.2 , pp. 1752-1765
    • Chatel-Chaix, L.1    Baril, M.2    Lamarre, D.3
  • 8
    • 84862816908 scopus 로고    scopus 로고
    • Recent progress in the development of selected hepatitis C virus NS3/4A protease and NS5B polymerase inhibitors
    • Kwong, A. D.; McNair, L.; Jacobson, I.; George, S. Recent progress in the development of selected hepatitis C virus NS3/4A protease and NS5B polymerase inhibitors. Curr. Opin. Pharmacol. 2008, 8, 522-531.
    • (2008) Curr. Opin. Pharmacol. , vol.8 , pp. 522-531
    • Kwong, A.D.1    McNair, L.2    Jacobson, I.3    George, S.4
  • 9
    • 84862161013 scopus 로고    scopus 로고
    • Treating hepatitis C: Current standard of care and emerging direct-acting antiviral agents
    • Poordad, F.; Dieterich, D. Treating hepatitis C: Current standard of care and emerging direct-acting antiviral agents. J. Viral Hepatitis 2012, 19, 449-464.
    • (2012) J. Viral Hepatitis , vol.19 , pp. 449-464
    • Poordad, F.1    Dieterich, D.2
  • 12
    • 77957663832 scopus 로고    scopus 로고
    • Drugs for hepatitis C: Unlocking a new mechanism of action
    • Bell, T. W. Drugs for Hepatitis C: Unlocking a New Mechanism of Action. ChemMedChem 2010, 5, 1663-1665.
    • (2010) ChemMedChem , vol.5 , pp. 1663-1665
    • Bell, T.W.1
  • 16
    • 0030939346 scopus 로고    scopus 로고
    • Use of the vinyl group as an efficient protecting group for azole N-atoms: Synthesis of polyfunctionalized imidazoles and thieno[2, 3-d]-[3, 2-d]imidazole
    • For an alternative synthesis of the thienoimidazole core, see Hartley, D. J.; Iddon, B. Use of the Vinyl Group as an Efficient Protecting Group for Azole N-Atoms: Synthesis of Polyfunctionalized Imidazoles and Thieno[2, 3-d]-[3, 2-d]imidazole. Tetrahedron Lett. 1997, 38, 4647-4650.
    • (1997) Tetrahedron Lett. , vol.38 , pp. 4647-4650
    • Hartley, D.J.1    Iddon, B.2
  • 17
    • 84990960457 scopus 로고    scopus 로고
    • See the Supporting Information for the details of the syntheses of intermediate 6 and compound 20
    • See the Supporting Information for the details of the syntheses of intermediate 6 and compound 20.
  • 18
    • 84990950262 scopus 로고    scopus 로고
    • Large potency drops were observed when 20 was screened against recombinant replicon cell lines harboring some of these mutations: (1a Y93H/C, >15000-fold; 1a M28T and Q30R >500-fold; and 1b Y93H, 900-fold)
    • Large potency drops were observed when 20 was screened against recombinant replicon cell lines harboring some of these mutations: (1a Y93H/C, >15000-fold; 1a M28T and Q30R >500-fold; and 1b Y93H, 900-fold).
  • 19
    • 77956116880 scopus 로고    scopus 로고
    • Resistance analysis of the hepatitis C virus NS5A inhibitor BMS-790052 in an in vitro replicon system
    • Fridell, R A; Qui, D.; Wang, C.; Valera, L.; Gao, M. Resistance Analysis of the Hepatitis C Virus NS5A Inhibitor BMS-790052 in an In Vitro Replicon System. Antimicrob. Agents Chemother. 2010, 54, 3641-3650.
    • (2010) Antimicrob. Agents Chemother , vol.54 , pp. 3641-3650
    • Fridell, R.A.1    Qui, D.2    Wang, C.3    Valera, L.4    Gao, M.5
  • 20
    • 84990949494 scopus 로고    scopus 로고
    • 50 of the positive control was within 40% of the mean value
    • 50 of the positive control was within 40% of the mean value.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.