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Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents

[Display omitted] In spired by the important role of amide groups of anti-influenza drugs oseltamivir, zanamivir and peramivir in bioactivity, a series of novel amides modified rupestonic acid derivatives were designed and synthesized. The absolute configuration of critical intermediate bearing chlo...

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Published in:Bioorganic & medicinal chemistry letters 2019-10, Vol.29 (19), p.126605-126605, Article 126605
Main Authors: Li, Gen, Obul, Mamateli, Zhao, Jiang-yu, Liu, Ge-yu, Lu, Wei, Aisa, Haji Akber
Format: Article
Language:English
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Summary:[Display omitted] In spired by the important role of amide groups of anti-influenza drugs oseltamivir, zanamivir and peramivir in bioactivity, a series of novel amides modified rupestonic acid derivatives were designed and synthesized. The absolute configuration of critical intermediate bearing chloride with newly formed stereocenter was confirmed by X-ray crystallographic analysis. And all new compounds were evaluated for their in vitro inhibitory activities against influenza A (H1N1 and H3N2) and influenza B viruses. The bioassay results showed that 5h with 4-fluorbenzylsulfonyl modified to 2 position of methyl rupestonate displayed the highest activity against influenza A (H1N1 and H3N2) viruses, even stronger than reference drugs oseltamivir and ribavirin (RVB), and might be recommended as a lead compound to further develop the new anti-influenza reagent.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.08.009