36775-95-8Relevant academic research and scientific papers
Discovery of Oxime Ethers as Hepatitis B Virus (HBV) Inhibitors by Docking, Screening and In Vitro Investigation
Tan, Jie,Zhou, Min,Cui, Xinhua,Wei, Zhuocai,Wei, Wanxing
, (2018)
A series of oxime ethers with C6-C4 fragment was designed and virtually bioactively screened by docking with a target, then provided by a Friedel-Crafts reaction, esterification (or amidation), and oximation from p-substituted phenyl derivatives (Methylbenzene, Methoxybenzene, Chlorobenzene). Anti-hepatitis B virus (HBV) activities of all synthesized compounds were evaluated with HepG2.2.15 cells in vitro. Results showed that most of compounds exhibited low cytotoxicity on HepG2.2.15 cells and significant inhibition on the secretion of HBsAg and HBeAg. Among them, compound 5c-1 showed the most potent activity on inhibiting HBsAg secretion (IC50 = 39.93 μM, SI = 28.51). Results of the bioactive screening showed that stronger the compounds bound to target human leukocyte antigen A protein in docking, the more active they were in anti-HBV activities in vitro.
With anti-hepatitis b virus activity of N - phenyl - 4 - phenyl d propionamide oxime and its derivatives (by machine translation)
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Paragraph 0031; 0033, (2017/04/27)
The present invention discloses an anti-hepatitis b virus activity of N - phenyl - 4 - phenyl d propionamide oxime and its derivatives, its structure is the following general formula: through the in vitro HepG2.2.15 cell activity experiment confirmed that, the invention N - phenyl - 4 - phenyl d propionamide oxime to the HBV surface antigen (HBsAg) e antigen (HBeAg) and has a certain inhibiting effect. Under the same conditions, the positive control drug lamivudine to HBsAg and HBeAg are respectively for the inhibition rate of 50.9% and 45.2%, while the compounds of this invention and the inhibition rate of the HBeAg HBsAg can reach 91.7% and 59.5%. Because this invention novel N - phenyl - 4 - phenyl d propionamide oxime with nucleoside similar medicine different structure, not only has significant effect of inhibiting HBV activity and low toxicity, are expected to be further developed into anti-hepatitis b virus of the new drug. (by machine translation)
BEHAVIOUR OF N-ARYLSUCCINISOIMIDIUM PERCHLORATES TOWARDS FRIEDEL-CRAFTS AND GRINGNARD REACTIONS
Ismail, Mohamed Fekry,Enayat, Ebtesam Ismail,El Bassiouny, Fakhry Abdel Aziz,Younes, Hamed Ahmed
, p. 103 - 108 (2007/10/02)
N-Arylsuccinisoimidium perchlorates (1a and b) reacted with aromatic hydrocarbons under Friedel-Crafts conditions to give β-aroyl-N-arylpriopionamides (3a-i).The reaction of phenylmagnesium bromide with 1a and 1b proceeded via ring-opening to give 3a and
