1-Phenyl-[2H]-tetrahydropyridazin-3-one, A-53612, a selective orally active 5-lipoxygenase inhibitor

Ring homologation of the known lipoxygenase inhibitor, phenidone to 1-phenyl-[2H]-tetrahydropyridazin-3-one provided A-53612, which was discovered to be a selective, orally active 5-lipoxygenase inhibitor. In contrast to phenidone, A-53612 did not cause significant inhibition of platelet 12-lipoxyge...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1992-11, Vol.2 (11), p.1353-1356
Main Authors: Brooks, Dee W., Albert, Daniel H., Dyer, Richard D., Bouska, Jennifer B., Young, Patrick, Rotert, Gary, Machinist, Joseph M., Carter, George W.
Format: Article
Language:English
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Summary:Ring homologation of the known lipoxygenase inhibitor, phenidone to 1-phenyl-[2H]-tetrahydropyridazin-3-one provided A-53612, which was discovered to be a selective, orally active 5-lipoxygenase inhibitor. In contrast to phenidone, A-53612 did not cause significant inhibition of platelet 12-lipoxygenase, soybean 15-lipoxygenase, or intact rat PMNL cyclo-oxygenase at concentrations up to 100 μM. Ring homologation of the known lipoxygenase inhibitor, phenidone (1) provided A-53612 (5), which was discovered to be a selective, orally active 5-lipoxygenase inhibitor.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)80511-9