title: Novel quinolizidine salicylamide influenza fusion inhibitors.
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 microg/mL in plaque reduction assay. The synthesis and the SAR of these compounds are discussed.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA.
authors.forename: K L
authors.initials: KL
authors.lastname: Yu
authors.forename: E
authors.initials: E
authors.lastname: Ruediger
authors.forename: G
authors.initials: G
authors.lastname: Luo
authors.forename: C
authors.initials: C
authors.lastname: Cianci
authors.forename: S
authors.initials: S
authors.lastname: Danetz
authors.forename: L
authors.initials: L
authors.lastname: Tiley
authors.forename: A K
authors.initials: AK
authors.lastname: Trehan
authors.forename: I
authors.initials: I
authors.lastname: Monkovic
authors.forename: B
authors.initials: B
authors.lastname: Pearce
authors.forename: A
authors.initials: A
authors.lastname: Martel
authors.forename: M
authors.initials: M
authors.lastname: Krystal
authors.forename: N A
authors.initials: NA
authors.lastname: Meanwell
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D002478:Cells, Cultured; D009980:Influenza A virus / Q000187:drug effects* / Q000502:physiology; D011807:Quinolizines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D012457:Salicylamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D011807:Quinolizines; D012457:Salicylamides