Structure-activity relationships for a series of thiobenzamide influenza fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine.
The anti-influenza activity of a series of thiobenzamide fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine is profiled. Axial disposition of the thioamide moiety is essential for potent influenza inhibitory activity.
Yu
Kuo Long
KL
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.
Torri
Albert F
AF
Luo
Guangxiang
G
Cianci
Christopher
C
Grant-Young
Katharine
K
Danetz
Stephanie
S
Tiley
Lawrence
L
Krystal
Mark
M
Meanwell
Nicholas A
NA
D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D006461:Hemolysis / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008561:Membrane Fusion / Q000187:drug effects; D008744:Methylamines / Q000737:chemistry* / Q000494:pharmacology*; D009975:Orthomyxoviridae / Q000187:drug effects*; D011807:Quinolizines / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013854:Thioamides / Q000737:chemistry* / Q000494:pharmacology*
D000998:Antiviral Agents; C105257:BMY 27709; D008744:Methylamines; D011807:Quinolizines; D013854:Thioamides; C015539:thiobenzamide; C027451:methylamine