Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors

…, T Kolasa, JD Ratajczyk, H Mazdiyasni…

Index: Stewart, Andrew O.; Bhatia, Pramila A.; Martin, Jonathan G.; Summers, James B.; Rodriques, Karen E.; Martin, Michael B.; Holms, James H.; Moore, Jimmie L.; Craig, Richard A.; Kolasa, Teodozyj; Ratajczyk, James D.; Mazdiyasni, Hormoz; Kerdesky, Francis A. J.; DeNinno, Shari L.; Maki, Robert G.; Bouska, Jennifer B.; Young, Patrick R.; Lanni, Carmine; Bell, Randy L.; Carter, George W.; Brooks, Clint D. W. Journal of Medicinal Chemistry, 1997 , vol. 40, # 13 p. 1955 - 1968

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Citation Number: 42

Abstract

The discovery of second generation N-hydroxyurea 5-lipoxygenase inhibitors was accomplished through the development of a broad structure-activity relationship (SAR) study. This study identified requirements for improving potency and also extending duration by limiting metabolism. Potency could be maintained by the incorporation of heterocyclic templates substituted with selected lipophilic substituents. Duration of inhibition after oral ...