Synthesis of Rupestonic Acid Derivatives with Antiviral Activity

Abstract

A series of 23 new rupestonic acid derivatives were synthesized. Their activities against influenza viruses A (H3N2, H1N1) and B were studied. Compounds 2d and 2g demonstrated potent activity against influenza virus A (H3N2) with IC50 values of 0.35 and 0.21 μM, respectively. Compound 5g (n = 10) was the most potent compound of this series against influenza viruses H3N2 and H1N1 with IC50 values of 2.89 and 0.38 μM. Several of the synthesized compounds were weakly active against influenza virus B and were more toxic than starting rupestonic acid.