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  • Title: Design, synthesis, and antihepatitis B virus activities of novel 2-pyridone derivatives.
    Author: Lv Z, Sheng C, Wang T, Zhang Y, Liu J, Feng J, Sun H, Zhong H, Niu C, Li K.
    Journal: J Med Chem; 2010 Jan 28; 53(2):660-8. PubMed ID: 20000776.
    Abstract:
    A series of novel 2-pyridone derivatives were synthesized and evaluated for their antihepatitis B virus (HBV) activity and cytotoxicity in vitro. Moderate to good activity against HBV DNA replication was observed in these 2-pyridone analogues. The most active compounds were 5d and 6l, with good inhibitory activity against HBV DNA replication (IC(50) = 0.206 and 0.12 microM, respectively) and remarkable high selectivity (selectivity indexes of >532 and 467, respectively). A pharmacophore model of the synthesized compounds was proposed by the GASP program. The pharmacophore model consists of three hydrophobic points, four HBA points, and one HBD point. The 2-pyridone derivatives represent a novel class of HBV inhibitors, which are worth further optimization.
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