Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.

@article{Huang2010BerberineDW,
  title={Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.},
  author={Ling Huang and Zonghua Luo and Feng He and Anding Shi and Fangfei Qin and Xingshu Li},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 22},
  pages={6649-52}
}
Berberine derivatives with substituted amino groups linked at the 9-position using different carbon spacers were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Compound 10b, with a cyclohexylamino group linked to berberine by a three carbon spacer, gave the most potent inhibitor activity with an IC(50) of 0.020 μM for AChE. Kinetic studies revealed mixed inhibition of AChE, and molecular modeling simulations of the AChE-inhibitor complex confirmed that… CONTINUE READING