Novel quinolizidine salicylamide influenza fusion inhibitors

A novel series of quinolizidine salicylamides was synthesized as specific i nhibitors of the H1 subtype of influenza A viruses. These inhibitors inhibi t the pH-induced fusion process, thereby blocking viral entry into host cel ls. Compound 16 was the most active inhibitor in this series with an EC50 o f 0.25 mu g/mL in plaque reduction assay. The synthesis and the SAR of thes e compounds are discussed. (C) 1999 Elsevier Science Ltd. All rights reserv ed.