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Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships

…, H Mazdiyasni, JH Holms, JD Ratajczyk…

文献索引:Summers; Kim; Mazdiyasni; Holms; Ratajczyk; Stewart; Dyer; Carter Journal of Medicinal Chemistry, 1990 , vol. 33, # 3 p. 992 - 998

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被引用次数: 65

摘要

An evaluation of the quantitative structureactivity relationships (QSAR) for more than 100 hydroxamic acids revealed that the primary physicochemical feature influencing the in vitro 5- lipoxygenase inhibitory potencies of these compounds is the hydrophobicity of the molecule. A significant correlation was observed between the octanol-water partition coefficient of the substituent attached to the carbonyl of the hydroxamate and in vitro inhibitory activity. This ...