Synthesis and structure–activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 3
Copyright policy )Synthesis and structure–activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 3
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). In particular, we investigated the possibility of introducing appropriate 1,11-O-benzylidene and 7-O-substituted benzoyl moieties into PPPA (1). The new o-substituted benzylidene derivatives showed higher selectivity for ACAT2 than PPPA (1). Among them, 1,11-O-o-methylbenzylidene-7-O-p-cyanobenzoyl PPPA derivative 7q and 1,11-O-o,o-dimethylbenzylidene-7-O-p-cyanobenzoyl PPPA derivative 7z proved to be potent ACAT2 inhibitors with unprecedented high isozyme selectivity.
- Wake Forest University United States
- Kitasato University Japan
Structure-Activity Relationship, Dose-Response Relationship, Drug, Molecular Structure, Sterol O-Acyltransferase 2, Pyridines, Humans, Enzyme Inhibitors, Sesquiterpenes, Sterol O-Acyltransferase
Structure-Activity Relationship, Dose-Response Relationship, Drug, Molecular Structure, Sterol O-Acyltransferase 2, Pyridines, Humans, Enzyme Inhibitors, Sesquiterpenes, Sterol O-Acyltransferase
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