Synthesis and structure-activity studies of some disubstituted phenylisoxazoles against human picornavirus.
A number of 2,6-disubstituted analogues of disoxaril, a broad spectrum antipicornavirus agent, have been prepared and evaluated against several rhinovirus serotypes. A QSAR study revealed that the mean MIC (MIC) against five rhinovirus serotypes correlated well with log P. The 2,6-dichloro analogue, 15, was highly effective in vitro against rhinoviruses with an MIC80 of 0.3 microM, as well as against several enteroviruses, and was also effective in preventing paralysis in mice infected with coxsackievirus A-9.
Diana
G D
GD
Sterling-Winthrop Research Institute, Rensselaer, New York 12144.
Cutcliffe
D
D
Oglesby
R C
RC
Otto
M J
MJ
Mallamo
J P
JP
Akullian
V
V
McKinlay
M A
MA
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003332:Coronaviridae / Q000187:drug effects*; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D010080:Oxazoles / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D007555:Isoxazoles; D010080:Oxazoles; C045978:disoxaril