Abstract
A series of pyripyropene A-based compounds were designed and synthesized by opening the upper section of the A-ring, which significantly simplifies the structure and synthesis from commercially available starting materials. Representative compound (-)-3 exhibited potent activity against ACAT2 and greater selectivity for ACAT2 than for ACAT1.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Drug Design*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Molecular Structure
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Pyridines / chemical synthesis
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Pyridines / chemistry
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Pyridines / pharmacology*
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Sesquiterpenes / chemical synthesis
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Sesquiterpenes / chemistry
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Sesquiterpenes / pharmacology*
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Sterol O-Acyltransferase / metabolism
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Sterol O-Acyltransferase 2
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Pyridines
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Sesquiterpenes
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pyripyropene A
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Sterol O-Acyltransferase