Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7230-7233

  Zhao, Yanfang ^a   Liu, Yajing ^a   Chen, Dong ^a   Wei, Zengquan ^a   Liu, Wenzhao ^a   Gong, Ping ^a  

^a SHENYANG PHARMACEUTICAL UNIVERSITY   (China)

Author keywords

1 Methyl 1H benzimidazol 5 ols; Anti HBV activity in vitro; Synthesis

Indexed keywords

ANTIVIRUS AGENT; BENZIMIDAZOLE DERIVATIVE; LAMIVUDINE; VIRUS DNA;

ANTIVIRAL ACTIVITY; ARTICLE; CELL STRAIN HEPG2; CYTOTOXICITY; DNA REPLICATION; DRUG POTENCY; DRUG SYNTHESIS; HEPATITIS B VIRUS; IC 50; NONHUMAN;

ANTIVIRAL AGENTS; BENZIMIDAZOLES; CELL LINE, TUMOR; DNA REPLICATION; HEPATITIS B VIRUS; HUMANS; LAMIVUDINE; STRUCTURE-ACTIVITY RELATIONSHIP;

HEPATITIS B VIRUS;

EID: 78449305467     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.099     Document Type: Article

References (17)

1. D. Ganem, and A.M. Prince N. Engl. J. Med. 350 2004 1118
2. P.E. Braz J. Infect. Dis. 12 2008 355
3. J.L. Dienstag N. Engl. J. Med. 359 2008 1486
4. J. Franco, and K.J. Saeian J. Vasc. Interv. Radiol. 13 2002 S191
5. E.J. Heathcote, E. Gane, and R. DeMan Hepatology 46 2007 861
6. F. Zoulim, D. Durantel, and P. Deny Liver Int. 29 2009 108
7. H.F. Chai, Y.F. Zhao, C.S. Zhao, and P. Gong Bioorg. Med. Chem. 14 2006 911
8. C.S. Zhao, Y.F. Zhao, H.F. Chai, and P. Gong Bioorg. Med. Chem. 14 2006 2552
9. C.S. Zhao, Y.F. Zhao, H.F. Chai, and P. Gong Chem. Res. Chin. Univ. 22 2006 577
10. Y.F. Zhao, R.L. Feng, Y.J. Liu, Y.K. Zhang, and P. Gong Chem. Res. Chin. Univ. 26 2010 272
11. Y.J. Liu, Y.F. Zhao, X. Zhai, X.S. Feng, J.X. Wang, and P. Gong Bioorg. Med. Chem. 16 2008 6522
12. Y.J. Liu, Y.F. Zhao, X. Zhai, X.P. Liu, L.X. Sun, Y.X. Ren, and P. Gong Arch. Pharm. 341 2008 446
13. Chen, D.; Liu, Y. J.; Zhang, S. L.; Guo, D. X.; Liu, C. H.; Li, S.; Gong, P. Arch. Pharm. in press.
14. -1: 3420.1, 2950.9, 1604.2, 1481.8, 1427.0, 1308.5, 1223.4, 1151.9, 1083.0, 803.4, 729.5. MS (ESI) m/z: 383.0 (M+H).
15. 50 and selected index of the evaluated compounds and lamivudine were calculated, respectively. Cytotoxicity assay: 2.2.15 cells were grown to confluence in 96-well flat-bottomed tissue culture plates and treated with tested compound (in 0.2 mL culture medium/well) as described above. Untreated control cultures were maintained on each 96-well plate. Toxicity was determined by measuring neutral red dye uptake, as determined from the cells' 510 nm absorbance relative to untreated cells, after the treatment of consecutive 9 days.
16. B.E. Korba, and J.L. Gerin Antiviral Res. 19 1992 55
17. B.E. Korba, and J.L. Gerin Antiviral Res. 28 1995 225