Bioorganic and Medicinal Chemistry Letters p. 2177 - 2180 (1999)
Update date:2022-08-05
Topics: Inhibitors Heterocyclic Influenza salicylamide fusion inhibitors
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.
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.
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