The search for new drugs synthesis and antiviral activity of derivatives of meristotropic and macedonic acids

Development of anti‐influenza agents from natural products

“…Among them, compounds 43 and 44 were the most active against H1N1 rimantadine-resistant virus A/PR/8/34 (CTD 50 = 683.7 μM), more potent than the reference rimantadine (CTD 50 = 379.8 μM), suggesting that they might have potential for further development as new effective anti-influenza drugs. 65 The bioactive triterpene saponin saikosaponin A (45) from Bupleurum chinense effectively attenuated IAV replication, including that of the highly pathogenic H5N1 strain, in human alveolar epithelial A549 cells via down regulation of both IAV-induced NF-κB activation and caspase 3-dependent NP nuclear translocation. Critically, it also protected against lethal PR8-induced mortality and morbidity in vivo through the reduction but not complete elimination of lung neutrophil and monocyte recruitment.…”

“…Two natural triterpenoid acids, meristotropic acid ( 43 ) and its methyl ester ( 44 ), as well as their synthetic derivatives, were tested for activities against influenza viruses A and B in MDCK cell cultures and a mouse model of lethal influenza pneumonia. Among them, compounds 43 and 44 were the most active against H1N1 rimantadine‐resistant virus A/PR/8/34 (CTD 50 = 683.7 μM), more potent than the reference rimantadine (CTD 50 = 379.8 μM), suggesting that they might have potential for further development as new effective anti‐influenza drugs 65 …”