《Synthesis and anti-HBV activity of novel 5-substituted pyridin-2(1H)-one derivatives》.pdfVIP

Available online at Chinese Chemical Letters 21 (2010) 290–292 /locate/cclet Synthesis and anti-HBV activity of novel 5-substituted pyridin-2(1H)-one derivatives CYi Kai Zhang, Zhi Liang Lv, Chun Juan Niu, Ke Li * H_NE5E Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China Received 6 July 2009 Abstract Four novel 5-substituted pyridine-2(1H)-one derivatives were designed and synthesized by using addition–elimination reactions. The structures of these novelly synthesized compounds were verified by 1H NMR, ESI-MS and single crystal X-ray diffraction. Furthermore, all four compounds (most notably compound 7a) were found to be highly efficient against hepatitis B virus (HBV) in cultured HepG2 2.2.15 cell, making them promising drug candidates for potential bioactive molecule against hepatitis B. # 2009 Ke Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. Keywords: 5-Substituted pyridin-2(1H)-one; Synthesis; Crystal structure; Anti-HBV activity Chronic hepatitis B virus (HBV) infection is a leading cause of liver cirrhosis and hepatocellular carcinoma and up to 1.2 million people die annually from HBV-related infection [1,2]. HBV is a member of the Hepadnavirus family and 口HEM_CAL the virus particle consists of an outer lipid envelope and an icosahedral nucleocapsid core. The nucleocapsid encloses the viral DNA and a DNA polymerase that has reverse transcriptase activity [3].