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• W2040399413 startingPage "8068" @default.
• W2040399413 abstract "Dual inhibition of the prostaglandin (PG) and leukotriene (LT) biosynthetic pathway is supposed to be superior over single interference, both in terms of efficacy and side effects. Here, we present a novel class of dual microsomal PGE2 synthase-1/5-lipoxygenase (5-LO) inhibitors based on the structure of pirinixic acid [PA, 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)acetic acid, compound 1]. Target-oriented structural modification of 1, particularly α substitution with extended n-alkyl or bulky aryl substituents and concomitant replacement of the 2,3-dimethylaniline by a biphenyl-4-yl-methane-amino residue, resulted in potent suppression of mPGES-1 and 5-LO activity, exemplified by 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid (7b, IC50 = 1.3 and 1 μM, respectively). Select compounds also potently reduced PGE2 and 5-LO product formation in intact cells. Importantly, inhibition of cyclooxygenases-1/2 was significantly less pronounced. Taken together, these pirinixic acid derivatives constitute a novel class of dual mPGES-1/5-LO inhibitors with a promising pharmacologial profile and a potential for therapeutic use." @default.
• W2040399413 created "2016-06-24" @default.
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• W2040399413 date "2008-11-19" @default.
• W2040399413 modified "2023-09-25" @default.
• W2040399413 title "Pirinixic Acid Derivatives as Novel Dual Inhibitors of Microsomal Prostaglandin E₂ Synthase-1 and 5-Lipoxygenase" @default.
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• W2040399413 doi "https://doi.org/10.1021/jm801085s" @default.
• W2040399413 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19053751" @default.
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