Chemical Modification of Rupestonic Acid and Preliminarily In Vitro Antiviral Activity Against Influenza A₃and B Viruses

Abstract

To improve the biological activities of rupestonic acid, 21 new rupestonic acid fatty ester derivatives (2a-2h) and aromatic ester derivatives (2i-2u) were synthesized and preliminarily evaluated for their anti-influenza activity in vitro by the national center for drug screening of China, using the Oseltamivir and Ribavirin as reference drugs. The results showed that 2l (<TEX>$IC_{50}=0.5{\mu}mol/L$</TEX>) exhibited potent anti-influenza <TEX>$A_3$</TEX> viral activity among the synthesized compounds and was 10-fold more potent than that of the reference drug Oseltamivir (<TEX>$IC_{50}=5.1{\mu}mol/L$</TEX>).