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Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors

[ Vol. 5 , Issue. 3 ]

Author(s):

John W. Clader   Pages 243 - 256 ( 14 )

Abstract:


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.

Keywords:

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

Affiliation:

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



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