In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase

JB Summers, BP Gunn, H Mazdiyasni…

Index: Summers, James B.; Gunn, Bruce P.; Mazdiyasni, Hormoz; Goetze, Andrew M.; Young, Patrick R.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 11 p. 2121 - 2126

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Citation Number: 72

Abstract

The hydroxamic acid functionality can be incorporated into simple molecules to produce potent inhibitors of 5-lipoxygenase. The ability of many of these hydroxamates to inhibit leukotriene synthesis in vivo has been measured directly with a rat peritoneal anaphylaxis model. Despite their potent enzyme inhibitory activity in vitro, many orally dosed hydroxamic acids only weakly inhibited leukotriene synthesis in vivo. This discrepancy is attributable ...