Novel quinolizidine salicylamide influenza fusion inhibitors

…, E Ruediger, G Luo, C Cianci, S Danetz, L Tiley…

Index: Yu, Kuo-Long; Ruediger, Edward; Luo, Guangxiang; Cianci, Christopher; Danetz, Stephanie; Tiley, Laurence; Trehan, Ashok K.; Monkovic, Ivo; Pearce, Bradley; Martel, Alain; Krystal, Mark; Meanwell, Nicholas A. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 15 p. 2177 - 2180

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Citation Number: 15

Abstract

A novel series of quinolizidine salicylamides was synthesized as specific inhibitors of the H1 subtype of influenza A viruses. These inhibitors inhibit the pH-induced fusion process, thereby blocking viral entry into host cells. Compound 16 was the most active inhibitor in this series with an EC50 of 0.25 μg/mL in plaque reduction assay. The synthesis and the SAR of these compounds are discussed.