Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors.

@article{Cavallaro2018AlkynylA,
  title={Alkynyl and β-ketophosphonates: Selective and potent butyrylcholinesterase inhibitors.},
  author={Val{\'e}ria Cavallaro and Yanina Moglie and Ana Paula Murray and Gabriel Radivoy},
  journal={Bioorganic chemistry},
  year={2018},
  volume={77},
  pages={
          420-428
        }
}
A series of thirty-three alkynyl and β-ketophosphonates were evaluated for their in vitro acetyl- and butyryl-cholinesterase (AChE and BChE) inhibitory activities using Ellman's spectrophotometric method. None of the examined compounds inhibited AChE activity at tested concentrations while twenty-nine of them showed significant and selective inhibition of BChE with IC50 values between 38.60 µM and 0.04 µM. In addition, structure-activity relationships were discussed. The most effective… CONTINUE READING

Topics from this paper.