Structure-activity relationships of the pyridazinone series of 5-lipoxygenase inhibitors

Structure activity analysis of the pyridazinone series as represented by the initial lead compound A-53612 revealed that the 1-phenyl-2H-tetrahydropyridazin-3-one structure was necessary for inhibitory activity as several modifications diverging from this structure led to a dramatic loss of inhibito...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters 1992-11, Vol.2 (11), p.1357-1360
Main Authors:	Brooks, Dee W., Basha, Anwer, Kerdesky, Francis A.J., Holms, James H., Ratajcyk, James D., Bhatia, Pramila, Moore, Jimmie L., Martin, Jonathan G., Schmidt, Steven P., Albert, Daniel H., Dyer, Richard D., Young, Patrick, Carter, George W.
Format:	Article
Language:	eng
Subjects:	Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
Online Access:	Get full text
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Summary:	Structure activity analysis of the pyridazinone series as represented by the initial lead compound A-53612 revealed that the 1-phenyl-2H-tetrahydropyridazin-3-one structure was necessary for inhibitory activity as several modifications diverging from this structure led to a dramatic loss of inhibitory activity. Substituents on the phenyl ring had a marked effect on inhibitory activity and methemoglobinemia toxicity. Structure-activity analysis of the pyridazinone series as represented by the initial lead compound A-53612 revealed that the 1-phenyl-2H-tetrahydropyridazin-3-one structure was necessary for 5-lipoxygenase inhibitory activity. Substituents on the phenyl ring had a marked effect on inhibitory activity and methemoglobinemia toxicity.
ISSN:	0960-894X 1464-3405