期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 1, 页码 101-104出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.09.078
关键词
backbone re-organized ezetimibe analogs; Azetidin-2-one; cholesterol absorption inhibition
The underlying principle of drug design in this paper is that the maximum retention of the functional groups that exist in the marketed drug would provide a higher probability for comparable safety while the conformational changes in the newly created analogs should not constitute a significant structural variation to adversely affect biological activity. Four individual isomers of backbone re-organized ezetimibe analogs were designed and synthesized. Their effects on the cholesterol levels in rat serum were evaluated by a high-cholesterol and high-fat diet feeding experiment. All the new analogs showed significant effect in lowering the levels of total cholesterol in serum. (c) 2006 Elsevier Ltd. All rights reserved.
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