Synthesis and evaluation of a new series of tri-, di-, and mono-N-alkylcarbamylphloroglucinols as bulky inhibitors of acetylcholinesterase.

@article{Lin2012SynthesisAE,
  title={Synthesis and evaluation of a new series of tri-, di-, and mono-N-alkylcarbamylphloroglucinols as bulky inhibitors of acetylcholinesterase.},
  author={Ming-Chen Lin and Gin-Zen Lin and Yu-Fong Shen and Shuo-Yung Jian and Dean-Kuo Hsieh and James Lin and Gialih Lin},
  journal={Chemical research in toxicology},
  year={2012},
  volume={25 7},
  pages={1462-71}
}
1,3,5-Tri-N-alkylcarbamylphloroglucinols (1-4) are synthesized as a new series of bulky inhibitors of acetylcholinesterase that may block the catalytic triad, the anionic substrate binding site, and the entrance of the enzyme simultaneously. Among three series of phloroglucinol-derived carbamates, tridentate inhibitors 1,3,5-tri-N-alkylcarbamylphloroglucinols (1-4), bidentate inhibitors 3,5-di-N-n-alkylcarbamyloxyphenols (5-8), and monodentate inhibitors 5-N-n-alkylcarbamyloxyresorcinols (9-12… CONTINUE READING