Antirhinoviral activity of heterocyclic analogs of Win 54954.
A variety of heterocyclic analogs of Win 54954 have been synthesized and tested in vitro against human rhinovirus type 14 (HRV-14) in a plaque reduction assay. The more active compounds were tested against 14 additional serotypes, and the concentration which inhibited 80% of the serotypes tested (MIC80) was measured. One compound, 37, exhibited activity comparable to Win 59454. Physicochemical as well as electrostatic parameters were calculated and the results subjected to a QSAR analysis in an effort to explain differences in activity observed between these compounds; however, no meaningful correlation with biological activity was found with any of these parameters.
Bailey
T R
TR
Sterling Winthrop Pharmaceutical Research Group, Rensselaer, New York 12144.
Diana
G D
GD
Kowalczyk
P J
PJ
Akullian
V
V
Eissenstat
M A
MA
Cutcliffe
D
D
Mallamo
J P
JP
Carabateas
P M
PM
Pevear
D C
DC
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004563:Electrochemistry; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D012229:Rhinovirus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000998:Antiviral Agents; D007555:Isoxazoles; D013777:Tetrazoles; C078822:5-(3,5-dichloro-4-((5-(3-methyl-5-isoxazolyl)pentyl)oxy)phenyl)-2-methyl-2H-tetrazole; C062554:Win 54954