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Synthesis and anti-influenza activity of aminoalkyl rupestonates
Zhao Jiangyu; Aisa Haji Akber; Aisa, HA
AbstractA 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.
KeywordRupestonic Acid Synthesis Anti-influenza Activity
Subject AreaPharmacology & Pharmacy ; Chemistry
Indexed BySCI
WOS IDWOS:000301285500041
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Cited Times:20[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Corresponding AuthorAisa, HA
AffiliationChinese 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
GB/T 7714
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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