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Title 

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

Authors 

Tae Sook JeongKyung Soon KimHana YuMi Jeong KimKyung Hyun ChoYang Kyu ChoiHyoung-Chin KimHo Yong ParkWoo Song Lee

Publisher 

Elsevier

Issue Date 

2005

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 2, pp. 385-388

Keywords 

ACAT inhibitorcholesterol acyltransferasecholesterol acyltransferase inhibitorhypocholesterolemic agentmanassantin Bsaucerneol bcholesterol dietdrug inhibitionenzyme inhibitionnonhuman

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2004.10.066

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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