Novel quinolizidine salicylamide influenza fusion inhibitors.
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.
Yu
K L
KL
Bristol-Myers Squibb Pharmaceutical Research Institute, Department of Chemistry, Wallingford, CT 06492, USA.
Ruediger
E
E
Luo
G
G
Cianci
C
C
Danetz
S
S
Tiley
L
L
Trehan
A K
AK
Monkovic
I
I
Pearce
B
B
Martel
A
A
Krystal
M
M
Meanwell
N A
NA
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
D000998:Antiviral Agents; D011807:Quinolizines; D012457:Salicylamides