Synthesis of Aurone Derivatives as Potential Anti-avian Flu Agents

碩士 === 國防醫學院 === 藥學研究所 === 97 === Avian influenza viruses (AIV) have become epidemic in some countries and continue to cause outbreaks in poultry and sporadic human infections since twenty century. The neuraminidase inhibitors oseltamivir and zanamivir are only clininicaly used to against AIV. AIV h...

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Bibliographic Details
Main Authors: Tsai, Su-Yu, 蔡素瑜
Other Authors: 李安榮
Format: Others
Language:zh-TW
Published: 2009
Online Access:http://ndltd.ncl.edu.tw/handle/69441191846554789613
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Summary:碩士 === 國防醫學院 === 藥學研究所 === 97 === Avian influenza viruses (AIV) have become epidemic in some countries and continue to cause outbreaks in poultry and sporadic human infections since twenty century. The neuraminidase inhibitors oseltamivir and zanamivir are only clininicaly used to against AIV. AIV have high variation and spread fast, so make efforts in developing novel drugs to against AIV is eager. Research studies have confirmed that aurones have antiviral, antifungal, and antioxidant properties. Synthesis of the 2-chloro ethanone intermediates was first formed by 3,5-dimethoxy phenol and chloroacetyl chloride in boron trifluoride diethyl etherate (Fries reaction). The 2-chloro ethanone was reacted with sodium carbonate in dry acetone undergoing cyclization to give benzofuranone. The benzofuranone treated with various benzaldehydes under basic condition such as potassium hydroxide in methanol to give a series of aurone derivatives. The target compounds will be subjected to evalutate antiviral activity. The ability of the synthetic aurones to interfere with the plaque formation by human influenza viruses was examined on the basis of the maximum non-toxic concentration of the test compounds. The preliminary screenings showed that compounds have two hydroxy groups have better inhibitory activity then others. A5、A6、A9、A11、A13、A14、A17、A19、A21 have potent inhibitory activity of influenza viruses(H1N1).