Adenine: an important drug scaffold for the design of antiviral agents

• 作者: Changyuan Wang Haiqing Yu Kexin Liu Xiaodong Ma Zhendong Song
• 来源期刊: 药学学报:英文版
• 学科: 医学
• 关键词: Antiviral Structureactivity relationship Adenine Aeyclic necleoside phosphonate Scaffold
• 年，卷（期）: 2015,（5）
• 页码范围: 431-441
• 页数: 11页
• 分类号: R91
• 语种: 中文

摘要

Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates(ANPS), possess signi fi cant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir(PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also wellknown anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modi fi cations on the scaffold itself and the peripheral sections were made.The structure-activity relationships(SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.