Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.

@article{Obata2000SyntheticCO,
  title={Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.},
  author={Rika Obata and Toshiaki Sunazuka and Kazuhiko Otoguro and Hiroshi Tomoda and Yoshihiro Harigaya and Satoshi O̅mura},
  journal={Bioorganic & medicinal chemistry letters},
  year={2000},
  volume={10 12},
  pages={1315-6}
}
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… CONTINUE READING