Author/Authors :
Keith D. Combrink، نويسنده , , H. Belgin Gulgeze، نويسنده , , Kuo-Long Yu، نويسنده , , Bradley C. Pearce، نويسنده , , Ashok K. Trehan، نويسنده , , Jianmei Wei، نويسنده , , Milind Deshpande، نويسنده , , Mark Krystal، نويسنده , , Albert Torri، نويسنده , , Guangxiang Luo، نويسنده , , Christopher Cianci، نويسنده , , Stephanie Danetz، نويسنده , , Laurence Tiley، نويسنده , , Nicholas A. Meanwell، نويسنده ,
Abstract :
Structural variation of the quinolizidine heterocycle of the influenza fusion inhibitor BMY-27709 was examined by several topological dissections in order 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 important for antiviral activity. The 2-methyl-cis-decahydroquinoline 6f was the most potent influenza inhibitor identified that demonstrated an EC50 of 90 ng/mL in a plaque reduction assay.
