Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
Basic Information
ID: ALA4373726
Journal: Bioorg Med Chem Lett
Title: Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.
Authors: Li G, Obul M, Zhao JY, Liu GY, Lu W, Aisa HA.
Abstract: 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.
CiteXplore: 31439378
DOI: 10.1016/j.bmcl.2019.08.009
Patent ID: ┄