synthesis of Functionalised derivatives of Pentaerythritol

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.

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

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

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.


2016 ◽  
Vol 36 (7) ◽  
pp. 1617
Author(s):  
Guangcan Xu ◽  
Qingchuan Liu ◽  
Jie Yuan ◽  
Zhanxing Hu ◽  
Fangfang Ma ◽  
...  

2014 ◽  
Vol 34 (5) ◽  
pp. 973 ◽  
Author(s):  
Guangping Liang ◽  
Peixue Cao ◽  
Xiuxia Yang ◽  
Zhengming Huang ◽  
Qingchuan Liu ◽  
...  

2006 ◽  
Vol 71 (7) ◽  
pp. 1122-1129 ◽  
Author(s):  
Minmin Yang ◽  
Tesfaye Serbessa ◽  
Stewart W. Schneller

The 3-deaza and 7-deaza derivatives of 5'-amino-5'-deoxy-5'-noraristeromycin (6 and 7, respectively) have been prepared from the common starting material (+)-(1R,4S)-4-hydroxycyclopent-2-en-1-yl acetate (8). Two Pd(0)-catalyzed allylic substitution reactions afforded the desired azide intermediates, 12 and 16, which were transformed to target compounds by standard procedures. These compounds were evaluated against a large number of viruses and found to be inactive except for weak effect against hepatitis B virus: 6, EC50 4.7 μM (3TC EC50 0.056 μM); 7, EC50 4.8 μM (3TC EC50 0.063 μM).


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