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学科主题: Pharmacology & Pharmacy ; Chemistry
题名: Synthesis and anti-influenza activity of aminoalkyl rupestonates
作者: Zhao Jiangyu; Aisa Haji Akber
通讯作者: Aisa, HA
关键词: Rupestonic acid ; Synthesis ; Anti-influenza activity
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2012
DOI: 10.1016/j.bmcl.2012.01.056
卷: 22, 期:6, 页:2321-2325
收录类别: SCI
摘要: A series of aminoalkyl rupestonates were designed and synthesized by reacting rupestonic acid with 1,omega-dibromoalkanes, followed by amination. All of the new compounds were bioassayed in vitro to determine their activities against influenza A (H3N2, H1N1) and B viruses. The results showed that compounds 5a-5g, which each contain a 1H-1,2,4-triazolyl moiety, were found to be the most potent set of compounds. Compound 5g was demonstrated to possess the highest inhibitory activity against influenza H3N2 and H1N1, with IC50 values of 0.97 and 0.42 mu M, respectively. Our results also indicated that compounds 2g, 3g, 4g and 5g, which contain ten-CH2-unit spacers between the rupestonic acid and amino functional groups, were the most potent inhibitors of influenza H1N1 among the synthesized compounds. Unfortunately, most of the synthesized compounds did not show an obvious activity against influenza B; the only exceptions were compounds 5d and 5f, which had IC50 values of 17.3 and 3.2 mu M, respectively. Compounds 4g and 5g were potent inhibitors of influenza H1N1, and they might be potentially developed as new lead anti-influenza virus compounds. Further studies of the mechanism of action are underway.
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内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/1635
Appears in Collections:新疆维吾尔自治区植物资源化学重点实验室 _期刊论文

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作者单位: Chinese Acad Sci, Key Lab Xinjiang Indigenous Med Plants Resource U, Xinjiang Tech Inst Phys & Chem, Urumqi 830011, Peoples R China;Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

Recommended Citation:
Zhao Jiangyu,Aisa Haji Akber. Synthesis and anti-influenza activity of aminoalkyl rupestonates[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(6):2321-2325.
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