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

Bioorg Med Chem Lett. 2005 Jan 17;15(2):385-8. doi: 10.1016/j.bmcl.2004.10.066.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acyl Coenzyme A / metabolism*
  • Animals
  • Anticholesteremic Agents / chemical synthesis*
  • Anticholesteremic Agents / pharmacology
  • Furans / chemical synthesis*
  • Furans / pharmacology
  • Humans
  • Keratinocytes / drug effects*
  • Keratinocytes / metabolism
  • Lignans / chemical synthesis*
  • Lignans / pharmacology
  • Mice
  • Sterol O-Acyltransferase / antagonists & inhibitors*
  • Sterol O-Acyltransferase / metabolism
  • Structure-Activity Relationship

Substances

  • Acyl Coenzyme A
  • Anticholesteremic Agents
  • Furans
  • Lignans
  • saucerneol B
  • Sterol O-Acyltransferase