1201816-84-3Relevant academic research and scientific papers
Design, synthesis, and antihepatitis B virus activities of novel 2-pyridone derivatives
Lv, Zhiliang,Sheng, Chunquan,Wang, Tiantian,Zhang, Yikai,Liu, Jia,Feng, Jilu,Sun, Hailing,Zhong, Hanyu,Niu, Chunjuan,Li, Ke
, p. 660 - 668 (2010)
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 (IC50 = 0.206 and 0.12 μM, 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 HBApoints, and one HBD point. The 2-pyridone derivatives represent a novel class of HBV inhibitors, which are worth further optimization. 2009 American Chemical Society.
