Abstract
In an effort to develop potent and selective inhibitors toward ACAT2, structure-activity relationship studies were carried out using derivatives based on pyripyropene A (PPPA, 1). We have successfully developed novel PPPA derivatives with a 7-O-substituted benzoyl substituent that significantly exhibit more potent ACAT2 inhibitory activity and higher ACAT2 isozyme selectivity than 1.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / chemistry*
-
Enzyme Inhibitors / pharmacology*
-
Pyridines / chemical synthesis
-
Pyridines / chemistry*
-
Pyridines / pharmacology*
-
Sesquiterpenes / chemical synthesis
-
Sesquiterpenes / chemistry*
-
Sesquiterpenes / pharmacology*
-
Sterol O-Acyltransferase / antagonists & inhibitors*
-
Sterol O-Acyltransferase 2
-
Structure-Activity Relationship
Substances
-
Enzyme Inhibitors
-
Pyridines
-
Sesquiterpenes
-
pyripyropene A
-
Sterol O-Acyltransferase