2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling.

@article{Delogu20162PhenylbenzofuranDA,
  title={2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling.},
  author={Giovanna Delogu and Maria Jo{\~a}o Matos and Maura Fanti and Benedetta Era and Rosaria Medda and Enrico Pieroni and Antonella Fais and Ashish Kumar and Francesca Pintus},
  journal={Bioorganic & medicinal chemistry letters},
  year={2016},
  volume={26 9},
  pages={2308-13}
}
A series of 2-phenylbenzofurans compounds was designed, synthesized and evaluated as cholinesterase inhibitors. The biological assay experiments showed that most of the compounds displayed a clearly selective inhibition for butyrylcholinesterase (BChE), while a weak or no effect towards acetylcholinesterase (AChE) was detected. Among these benzofuran derivatives, compound 16 exhibited the highest BChE inhibition with an IC50 value of 30.3 μM. This compound was found to be a mixed-type inhibitor… CONTINUE READING
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