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Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors

[ Vol. 5 , Issue. 3 ]


John W. Clader   Pages 243 - 256 ( 14 )


Atherosclerotic coronary artery disease remains a major healthcare concern especially in developed countries. While lowering plasma cholesterol levels via diet, exercise, and pharmacoptherapy can reduce this risk of developing coronary artery disease, there remains a need for more effective drug therapies. The azetidinone cholesterol absorption inhibitors typified by ezetimibe represent the first new approach to lipid lowering therapy in more than a decade. This review summarizes the medicinal chemistry of the azetidinone cholesterol absorption inhibitors as a class, with emphasis on factors that contributed both to the discovery of ezetimibe as well as to our overall understanding of S.A.R. trends in this area.


coronary artery disease, hypercholesterolemia, ldl, acat inhibitor, azetidinones, serum cholesterol (sc), pharmacophore


Department of Cardiovascular and CNS Medicinal Chemistry, Schering-Plough Research Institute, 2015Galloping Hill Road, Kenilworth, NJ 07033-1300, USA.

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