Optimization of benzoquinone and hydroquinone derivatives as potent inhibitors of human 5-lipoxygenase

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• 作者：Antonella Peduto^a ; ^f ; ¹ ; Maria Scuotto^a ; ¹ ; Verena Krauth^b ; ¹ ; Fiorentina Roviezzo^c ; Antonietta Rossi^c ; Veronika Temml^d ; Veronica Esposito^c ; Hermann Stuppner^d ; Daniela Schuster^e ; Bruno D'Agostino^a ; Chiara Schiraldi^a ; Mario de Rosa^a ; Oliver Werz^b ; ^{oliver.werz@uni-jena.de} ; Rosanna Filosa^a ; ^f ; ^{rosanna.filosa@unina2.it}
• 关键词：5-Lipoxygenase ; Quinones
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：715-726
• 全文大小：3125 K
• 卷排序：127

文摘

Three synthetic ubiquinol compounds had an IC50 value in the range of nanomolar, in active neutrophils. Compound 30 (1mg/kg i.p.) potently suppressed the levels of cysteinyl-LTs. Docking analysis predicted a binding of inhibitors to the enzyme-substrate complex.