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,...

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Veröffentlicht in:	Journal of medicinal chemistry 1989-02, Vol.32 (2), p.450-455
Hauptverfasser:	Diana, Guy D, Cutcliffe, David, Oglesby, Richard C, Otto, Michael J, Mallamo, John P, Akullian, Vahan, McKinlay, Mark A
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral Agents - chemical synthesis Antiviral Agents - pharmacology Chemistry Coronaviridae - drug effects enterovirus Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Humans Isoxazoles - chemical synthesis Isoxazoles - pharmacology Organic chemistry Oxazoles - chemical synthesis Preparations and properties rhinovirus Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00122a027