Dioxolane cytosine nucleosides as anti-hepatitis B agents

✍ Scribed by Migyoung Lee; Chung K. Chu; S. Balakrishna Pai; Yong-Lian Zhu; Yung-Chi Cheng; Moon Woo Chun; Won Keun Chung

• Book ID: 103983059
• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 231 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00343-r

✦ Synopsis

In order to study the structure-activity relationships, several dioxolane pyrimidine nucleosides have been synthesized and their anti-HBV activities have been evaluated in 2.2.15 cells. From the study it was found that 5-fluoro-cytosine derivatives exhibited the most potent anti-HBV activity.

Recently, several nucleosides have been reported as potent antiviral agents against human hepatitis B virus (HBV). These include 13-L-(2-hydroxymethyl-l,3-oxathiolan-4-yl)cytosine (3TC),I ~L-(2-hydroxymethyl-l,3oxathiolan-4-yl)-5-fluorocytosine (FrC),2 ~L-2',3'-dideoxy-5-fluoro-cytidine (L-FddC),3, 4 2'-fluoro-5-methyl-~-L-arahinofuranosyluracil (L-FMAU),5 and ~-D-9-(2-hydroxymethyl-1,3-dioxolan-4-yl)-2,6-diaminopurine (DAPD).6 These nucleosides are currently undergoing preclinicai and clinical studies as anti-HBV agents (Figure 1).