Analogs of arachidonic acid methylated at C-7 and C-10 as inhibitors of leukotriene biosynthesis |
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| Authors: | N Cohen G Weber BL Banner AF Welton WC Hope H Crowley WA Anderson BA Simko M O'Donnell JW Coffey C Fiedler-Nagy C Batula-Bernardo |
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| Institution: | 1. Department of Medicinal Chemistry Hoffmann-La Roche Inc. Nutley, New Jersey 07110, USA;1. Department of Pharmacology Hoffman-La Roche Inc. Nutley, New Jersey 07110, USA |
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| Abstract: | The syntheses and biological activity of (all
)-7,7-dimethyl-5-8,- 11,14-eicosatetraenoic acid, (all
)-7,7,-dimethyl-5,8,11-eicosatrienoic acid, (
,
-7,7-dimethyl-5,8-eicosadienoic acid, (all
)-10,10-dimetyl- 5,8,11,14-eicosatetraenoic acid, (all
-10,10-dimethyl-5,8,11-eicosatrienoic acid, and
.-(
,
-15-hydroxy-7,7-dimethyl-5,8-eicosadienoic acid are described. These arachidonic acid analogs are all inhibitors of ionophore-induced SRS-A biosynthesis in rat peritoneal cells. Their mode of action may involve inhibition of phospholipase A2 rather than Δ5-lipoxygenase. These compounds failed to exhibit significant activity in an
model designed to detect inhibitors of antigen-induced, leukotriene-mediated bronchoconstriction is sensitized guinea pigs. |
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| Keywords: | |
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