Encouraging Effects of Ethacrynic Acid Derivatives Possessing a Privileged ???±, ???2-Unsaturated Carbonyl Structure Scaffold

摘要

α, β-unsaturated carbonyl unit has remarkable utility in the development of biologically active and therapeutically relevant compounds in medicinal chemistry. In recent years, a number of Ethacrynic acid (EA) derivatives containing α, β-unsaturated carbonyl group were reported, which displayed versatile biological activities, such as antitumor activity, antimalarial effects, antiviral activity and reducing intraocular pressure. In this review, we summed up a number of derivatives regarding Ethacrynic acid as the lead and α, β-unsaturated carbonyl moiety as the functional group, researching on structure-activity relationship and evaluating their various biological activities in recent years. By summarizing the structure-activity relationships of these derivatives, we aimed to demonstrate α, β-unsaturated carbonyl group is a privileged scaffold in these structures and we should pay more attention to α, β-unsaturated carbonyl group to the development of more effectively bioactive new compounds.'.