Design, synthesis and biological evaluation of novel l-ascorbic acid-conjugated pentacyclic triterpene derivatives as potential influenza virus entry inhibitors
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- 作者：Han Wanga ; 1 ; Renyang Xua ; 1 ; Yongying Shia ; Longlong Sia ; Pingxuan Jiaoa ; Zibo Fana ; Xu Hana ; Xingyu Wub ; Xiaoshu Zhoua ; Fei Yua ; c ; Yongmin Zhangd ; Liangren Zhanga ; Lihe Zhanga ; Demin Zhoua ; deminzhou@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Sulong Xiaoa ; slxiao@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Influenza virus ; Pentacyclic triterpene ; l-ascorbic acid ; Entry inhibitor ; Hemagglutinin ; Sialic acid receptor
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：376-388
- 全文大小：1827 K
文摘
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A total of 20 l-ascorbic acid-conjugated pentacyclic triterpene derivatives were synthesized.
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The anti-influenza activities of those conjugates were evaluated.
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Compound 30 displayed the highest anti-influenza A/WSN/33 (H1N1) activity with an IC50 at 8.7 µM.
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Mechanistic studies indicated that compound 30 could tightly bind with HA protein (KD = 3.76 μM).