Synthesis and antiviral bioactivity of novel (1E, 4E)-1-aryl-5-(2-(quinazolin-4-yloxy)phenyl)-1,4-pentadien-3-one derivatives

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• 作者：Hui Luo ; Jiaju Liu ; Linhong Jin ; Deyu Hu ; ^{fcc.dyhu@gzu.edu.cn} ; Zhen Chen ; Song Yang ; Jian Wu ; Baoan Song ; ^{songbaoan22@yahoo.com}
• 关键词：(1E ; 4E)-1 ; 4-Pentadien-3-one derivatives ; Quinazoline moiety ; Tobacco mosaic virus ; Cucumber mosaic virus ; Antiviral activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：May, 2013
• 年：2013
• 卷：63
• 期：Complete
• 页码：662-669
• 全文大小：426 K

文摘

A series of novel (1E, 4E)-1-aryl-5-[2-(quinazolin-4-yloxy)phenyl]-1,4-pentadien-3-one derivatives were designed and synthesized by reacting substituent aldehyde with intermediates 4a-f. Antiviral bioassays indicated that most of the compounds exhibited promising ex?vivo antiviral bioactivities against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) at 500?¦Ìg/mL. The relationship between structure and antiviral activity was also discussed. Compounds 5a, 6e, and 6g could possess appreciable protective bioactivities on TMV ex?vivo by approximately 50 % (EC₅₀) at 257.7, 320.7 and 243.3?¦Ìg/mL. This study is the first to demonstrate that (1E, 4E)-1-aryl-5-(2-(quinazolin-4-yloxy)phenyl)-1,4-pentadien-3-one can be used to develop potential virucides for plants.