Design, Synthesis, and Evaluation of Novel 2-Substituted 3-Hydroxypyridin-4-ones: Structure-Activity Investigation of Metalloenzyme Inhibition by Iron Chelators §

ZD Liu, R Kayyali, RC Hider, JB Porter…

Index: Liu, Zu D.; Kayyali, Reem; Hider, Robert C.; Porter, John B.; Theobald, Anthony E. Journal of Medicinal Chemistry, 2002 , vol. 45, # 3 p. 631 - 639

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Citation Number: 58

Abstract

A range of novel 3-hydroxypyridin-4-ones with different R2 substitutents has been synthesized for the investigation of the structure-activity relationship between the chemical nature of the ligand and the inhibitory activity of the iron-containing metalloenzyme 5- lipoxygenase. Results indicate that the molecular dimensions, together with the lipophilicity, have a critical impact on the ability of this class of chelator to inhibit 5-lipoxygenase. ...