Abstract
In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.
Highlights
Atherosclerotic coronary heart disease (CHD) has been the major cause of death and cardiovascular morbidity in the world [1]
The prominent risk factor associated with CHD was the elevation of serum cholesterol levels [2]
The synthetic route to 2a-d is summarized in Scheme 1 [12]
Summary
Atherosclerotic coronary heart disease (CHD) has been the major cause of death and cardiovascular morbidity in the world [1]. Well established clinical treatment for CHD has focused on life style changes and the reduction of serum cholesterol. These reductions have been shown to correlate strongly with the decrease of CHD mortality and the reversal of atherosclerosis as evidenced by the regression of occlusion of coronary arteries [3]. These reductions have focused on the use of “statins” or HMG-CoA reductase inhibitors to affect both the biosynthesis of cholesterol and clearance mechanisms [4]. The ezetimibe analogs 2a-d and 3a-d (Fig. 1) were designed, synthesized and their ability to inhibit cholesterol absorption was evaluated [11]
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