Design and Synthesis of 5??Lipoxygenase Inhibitors

M Strasser, P Cooper, B Dewald…

Index: Strasser; Cooper; Dewald; Payne Helvetica Chimica Acta, 1988 , vol. 71, # 5 p. 1156 - 1176

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Citation Number: 12

Abstract

Abstract Based on the substrate specificity for 5-lipoxygenase and the known stereochemical course of the reaction, a hypothetical model of the enzyme active site was developed and used to design 2 types of selective inhibitors of 5-lipoxygenase. Both inhibitor types used aromatic rings in place of (Z)-olefins of the substrate and were designed to mimic the nonpolar end of arachidonic acid. One inhibitor type used a carboxylic-acid ...