New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.

@article{Sauvatre2007NewPA,
  title={New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series.},
  author={Thibault Sauva{\^i}tre and Mireille Barlier and Denyse Herlem and Nohad Gresh and Ang{\`e}le Chiaroni and Daniel Gu{\'e}nard and Catherine Guillou},
  journal={Journal of medicinal chemistry},
  year={2007},
  volume={50 22},
  pages={5311-23}
}
A new highly selective inhibitor of acetylcholinesterase (AChE) was discovered by high-throughput screening. Compound 1 was synthesized from a natural product, the N-3-isobutyrylcycloxobuxidine-F 2. A new extraction protocol of this compound is described. The hemisynthesis and optimization of 1 are reported. The analogs of 1 were tested in vitro for the inhibition of both cholinesterases (AChE and BuChE). These compounds selectively inhibited AChE. Extensive molecular docking studies were… CONTINUE READING

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