PMID: 2502629Aug 1, 1989Paper

Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis

Journal of Medicinal Chemistry
F C HuangP A Sonnino

Abstract

The synthesis of a series of novel substituted hydroxamates has been described along with their profile of inhibitory activity against 5-lipoxygenase, 12-lipoxygenase, and cyclooxygenase enzymes. The structure--activity relationship suggests that future molecules could be designed to specifically inhibit one or more of these enzymes since there were definite differences in structure--activity relationships for these different enzymes. A representative number of these compounds have been tested in vivo and found to possess potent oral activity in a systemic anaphylaxis model mediated by leukotrienes and topical activity in an arachidonic acid induced inflammation model. One of these molecules, compound 20, demonstrated that a leukotriene antagonist pharmacophore can be modified such that it contains both antagonist activity and 5-lipoxygenase inhibitory activity.

Citations

Nov 15, 1994·Annals of the New York Academy of Sciences·D G Tang, K V Honn
Nov 7, 2002·Biological & Pharmaceutical Bulletin·Hiromi KataokaYoshio Ito
Nov 4, 2000·Expert Opinion on Investigational Drugs·V E SteeleG J Kelloff
Dec 14, 2004·Prostaglandins, Leukotrienes, and Essential Fatty Acids·Jun MaSharon G Adler
Apr 9, 2008·World Journal of Gastroenterology : WJG·Pornprom YoysungnoenSuthiluk Patumraj
Oct 14, 2009·Journal of Medicinal Chemistry·Marion FlipoRebecca Deprez-Poulain

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Anaphylaxis is a serious allergic reaction that is rapid in onset and may cause death.