Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 17, Pages 5449-5453Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800588x
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Funding
- EU [LSHM-CT-2004-00533]
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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, compound 1) is presented. Systematic profilin g, of 1, i.e., esterification of the carboxylic acid, cc-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 ethyl 2-[4-chloro-6-(quinoline-6-ylamino)-pyrimidin-2-ylsulfanyl]octane-1-carboxylate (6d, IC50 = 0.6 mu M). These derivatives may possess potential for intervention with inflammatory and allergic diseases.
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