Author/Authors :
Rika Obata، نويسنده , , Toshiaki Sunazuka، نويسنده , , Kazuhiko Otoguro، نويسنده , , Hiroshi Tomoda، نويسنده , , Yoshihiro Harigaya، نويسنده , , Satoshi mura، نويسنده ,
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 γ-acylation/cyclization with several aroyl chlorides. The 4-pyridyl analogue selectively showed AChE inhibitory activity (IC50=7.9 μM) and no ACAT inhibitory activity IC50=>1000 μM.