Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors

Author(s): John W. Clader

Journal Name: Current Topics in Medicinal Chemistry

Volume 5 , Issue 3 , 2005

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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

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Article Details

Year: 2005
Page: [243 - 256]
Pages: 14
DOI: 10.2174/1568026053544498
Price: $65

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