[摘要]：A novel class of potent 5-lipoxygenase (5-LO) product synthesis inhibitors based on the structure of pirinixic acid (4-chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid, compd. 1) is presented. Systematic profiling of 1, i.e., esterification of the carboxylic acid, a-substitution, and replacement of the o-dimethylaniline by 6-aminoquinoline, leads to potent suppressors of 5-LO product formation in activated polymorphonuclear leukocytes, exemplified by Et 2-[4-chloro-6-(quinoline-6-ylamino)-pyrimidin-2-ylsulfanyl]octane-1-carb oxylate (6d, IC50 = 0.6 mM). These derivs. may possess potential for intervention with inflammatory and allergic diseases.
