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Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor
R Obata1, T Sunazuka, K Otoguro
1Research Center for Biological Function, The Kitasato Institute and Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Bioorganic & Medicinal Chemistry Letters
|July 13, 2000
Abstract:
Natural product acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor pyripyropene A was synthetically converted to acetylcholinesterase (AChE) inhibitor via heterolitic cleavage of the 2-pyrone ring, followed by gamma-acylation/cyclization with several aroyl chlorides. The 4-pyridyl analogue selectively showed AChE inhibitory activity (IC50 7.9 microM) and no ACAT inhibitory activity IC50 = >1000 microM.