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
Current Topics in Medicinal Chemistry
Title: Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors
Volume: 5 Issue: 3
Author(s): John W. Clader
Affiliation:
Keywords: coronary artery disease, hypercholesterolemia, ldl, acat inhibitor, azetidinones, serum cholesterol (sc), pharmacophore
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.
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Cite this article as:
Clader W. John, Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors, Current Topics in Medicinal Chemistry 2005; 5 (3) . https://dx.doi.org/10.2174/1568026053544498
DOI https://dx.doi.org/10.2174/1568026053544498 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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