Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors

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• 作者：Sebastien Boucle^a ; Xiao Lu^a ; Leda Bassit^a ; Tugba Ozturk^a ; Olivia Ollinger Russell^a ; Franck Amblard^a ; Steven J. Coats^b ; Raymond F. Schinazi^a ; ^{rschina@emory.edu}
• 关键词：HBV ; HAP ; Heteroarylpyrimidine ; Capsid assembly effectors
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：904-910
• 全文大小：1923 K
• 卷排序：27

文摘

New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range.