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Bioorg Med Chem Lett. 2013 Jul 1;23(13):3798-801. doi: 10.1016/j.bmcl.2013.04.075. Epub 2013 May 8.

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 3.

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  • 1Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Tokyo 108-8641, Japan.


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.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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