| Title | Synthesis and Anti-HBV Activities Evaluation of New Ethyl 8-Imidazolylmethyl-7-hydroxyquinoline-3-carboxylate Derivatives in vitro. | | Author(s) | Liu Y, Zhao Y, Zhai X, Liu X, Sun L, Ren Y, Gong P | | Institution | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China. Fax: +86 24 2398‐6429. | | Source | Arch Pharm (Weinheim) 2008 Jun 24. | | Abstract | Some new ethyl 8-imidazolylmethyl-7-hydroxyquinoline-3-carboxylate derivatives have been synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in HepG2.2.15 cells stable transfection with HBV. Compounds 13a, 11b, 11c, 12c, 13c, 11g, and 12g inhibited the expression of the viral antigens HBsAg or HBeAg in a low concentration, of which 11c (IC(50 )= 12.6 muM, SI = 12.4), 12c (IC(50 )= 3.5 muM, SI = 37.9), and 12g (IC(50) = 2.6 muM, SI = 61.6) showed more active abilities to inhibit the replication of HBV DNA than the positive control lamivudine (3TC, IC(50) = 343.2 muM, SI = 7.0). | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 18574853 |
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