scholarly journals Design, Synthesis and Bioactive Evaluation of Oxime Derivatives of Dehydrocholic Acid as Anti-Hepatitis B Virus Agents

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3359
Author(s):  
Zhuocai Wei ◽  
Jie Tan ◽  
Xinhua Cui ◽  
Min Zhou ◽  
Yunhou Huang ◽  
...  

Oxime derivatives of dehydrocholic acid and its esters were designed for anti-hepatitis B virus (HBV) drugs according to principles of assembling active chemical fragments. Twelve compounds were synthesized from dehydrocholic acid by esterification and oxime formation, and their anti-hepatitis B virus (HBV) activities were evaluated with HepG 2.2.15 cells. Results showed that 5 compounds exhibited more effective inhibition of HBeAg than positive control, among them 2b-3 and 2b-1 showed significant anti-HBV activities on inhibiting secretion of HBeAg (IC50 (2b-3) = 49.39 ± 12.78 μM, SI (2b-3) = 11.03; IC50 (2b-1) = 96.64 ± 28.99 μM, SI (2b-1) = 10.35) compared to the Entecavir (IC50 = 161.24 μM, SI = 3.72). Molecular docking studies showed that most of these compounds interacted with protein residues of heparan sulfate proteoglycan (HSPG) in host hepatocyte and bile acid receptor.

2015 ◽  
Vol 11 (2) ◽  
pp. 165-179 ◽  
Author(s):  
Li-Jun Wang ◽  
Hao Chen ◽  
Yun-Bao Ma ◽  
Xiao-Yan Huang ◽  
Chang-An Geng ◽  
...  

2018 ◽  
Vol 144 ◽  
pp. 424-434 ◽  
Author(s):  
Jingying Qiu ◽  
Qineng Gong ◽  
Jian Gao ◽  
Wang Chen ◽  
Yinpeng Zhang ◽  
...  

2011 ◽  
Vol 21 (7) ◽  
pp. 1179-1187 ◽  
Author(s):  
Di Wu ◽  
Jun-Qi Niu ◽  
Yan-Hua Ding ◽  
Xin-Yu Wu ◽  
Bo-Hua Zhong ◽  
...  

2003 ◽  
Vol 2003 (1) ◽  
pp. 2-3 ◽  
Author(s):  
E. S. H. El Ashry ◽  
Y. El Kilany ◽  
H. Abdel Hamid ◽  
S. R. El-Zemity ◽  
S. Boghdady

The synthesis of functionalised derivatives of pentaerythritol has been attempted by the reaction of 1 with different aldehydes and nucleophilic reagents; the activity of various derivatives against hepatitis B virus has been studied.


2016 ◽  
Vol 123 ◽  
pp. 202-210 ◽  
Author(s):  
Haiyong Jia ◽  
Fuxiang Bai ◽  
Na Liu ◽  
Xiaohong Liang ◽  
Peng Zhan ◽  
...  

2012 ◽  
Vol 54 ◽  
pp. 352-365 ◽  
Author(s):  
Li-Jun Wang ◽  
Chang-An Geng ◽  
Yun-Bao Ma ◽  
Jie Luo ◽  
Xiao-Yan Huang ◽  
...  

1989 ◽  
Vol 42 (4) ◽  
pp. 644-646 ◽  
Author(s):  
TAKEMITSU NAGAHATA ◽  
KEIJI UEDA ◽  
TOSHIKI TSURIMOTO ◽  
OSAMU CHISAKA ◽  
KENICHI MATSUBARA

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