Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors

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.

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