Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors

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Title
Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors
Author(s)
Tae Sook Jeong; Kyung Soon Kim; Hana Yu; Mi Jeong Kim; Kyung Hyun Cho; Yang Kyu Choi; Hyoung-Chin KimHo Yong ParkWoo Song Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 2, pp. 385-388
Publication Year
2005
Abstract
A series of saucerneol B derivatives 2a-i were prepared for evaluating their acyl-CoA: cholesterol acyltransferase inhibitory activities. Compounds 2a-g showed more specificity of hACAT-1 than hACAT-2. Saucerneol B (1) exhibited strong cholesterol-lowering effect in high cholesterol-fed mice. A series of 2a-i were prepared from a lead compound, saucerneol B (1) for evaluating their acyl-CoA: cholesterol acyltransferase inhibitory activities. Compounds 2a-g exhibited the high specificity of hACAT-1 than hACAT-2, whereas 2h and 2i showed very weak inhibitory activities in both hACAT-1 and hACAT-2. Saucerneol B (1) exhibited strong cholesterol-lowering effect in high cholesterol-fed mice.
Keyword
ACAT inhibitor
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2004.10.066
Type
Article
Appears in Collections:
Division of Biomaterials Research > Industrial Bio-materials Research Center > 1. Journal Articles
Ochang Branch Institute > Division of Bioinfrastructure > 1. Journal Articles
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
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