Salicylamide inhibitors of influenza virus fusion

Structural variation of the quinolizidine heterocycle of the influenza fusi on inhibitor BMY-27709 was examined by several topological dissections in o rder to illuminate the critical features of the ring system. This exercise resulted in the identification of a series of synthetically more accessible decahydroquinolines that retained the structural elements of BMY-27709 imp ortant for antiviral activity. The 2-methyl-cis-decahydroquinoline 6f was t he most potent influenza inhibitor identified that demonstrated an EC50 of 90 ng/mL in a plaque reduction assay. (C) 2000 Elsevier Science Ltd. All ri ghts reserved.