Design, synthesis and biological evaluation of novel l-ascorbic acid-conjugated pentacyclic triterpene derivatives as potential influenza virus entry inhibitors

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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 Wang^a ; ¹ ; Renyang Xu^a ; ¹ ; Yongying Shi^a ; Longlong Si^a ; Pingxuan Jiao^a ; Zibo Fan^a ; Xu Han^a ; Xingyu Wu^b ; Xiaoshu Zhou^a ; Fei Yu^a ; ^c ; Yongmin Zhang^d ; Liangren Zhang^a ; Lihe Zhang^a ; Demin Zhou^a ; ^{deminzhou@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Sulong Xiao^a ; ^{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

•: A total of 20 l-ascorbic acid-conjugated pentacyclic triterpene derivatives were synthesized.
•: The anti-influenza activities of those conjugates were evaluated.
•: Compound 30 displayed the highest anti-influenza A/WSN/33 (H1N1) activity with an IC₅₀ at 8.7 µM.
•: Mechanistic studies indicated that compound 30 could tightly bind with HA protein (K_D = 3.76 μM).