Synthesis and anti-influenza activity of aminoalkyl rupestonates
Zhao Jiangyu; Aisa Haji Akber; Aisa, HA
2012
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号22期号:6页码:2321-2325
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.
关键词Rupestonic Acid Synthesis Anti-influenza Activity
学科领域Pharmacology & Pharmacy ; Chemistry
DOI10.1016/j.bmcl.2012.01.056
收录类别SCI
WOS记录号WOS:000301285500041
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被引频次:19[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.xjipc.cas.cn/handle/365002/1635
专题省部共建新疆特有药用资源利用重点实验室
通讯作者Aisa, HA
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
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Zhao Jiangyu,Aisa Haji Akber,Aisa, HA. Synthesis and anti-influenza activity of aminoalkyl rupestonates[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(6):2321-2325.
APA Zhao Jiangyu,Aisa Haji Akber,&Aisa, HA.(2012).Synthesis and anti-influenza activity of aminoalkyl rupestonates.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(6),2321-2325.
MLA Zhao Jiangyu,et al."Synthesis and anti-influenza activity of aminoalkyl rupestonates".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.6(2012):2321-2325.
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