New structural scaffolds for centrally acting oxime reactivators of phosphylated cholinesterases.

@article{Sit2011NewSS,
  title={New structural scaffolds for centrally acting oxime reactivators of phosphylated cholinesterases.},
  author={Rakesh K. Sit and Zoran Radic and Valeria Gerardi and Limin Zhang and Edzna Garcia and Maja Katalini{\'c} and Gabriel Amitai and Zrinka Kovarik and Valery V Fokin and K. Barry Sharpless and Palmer Taylor},
  journal={The Journal of biological chemistry},
  year={2011},
  volume={286 22},
  pages={19422-30}
}
We describe here the synthesis and activity of a new series of oxime reactivators of cholinesterases (ChEs) that contain tertiary amine or imidazole protonatable functional groups. Equilibration between the neutral and protonated species at physiological pH enables the reactivators to cross the blood-brain barrier and distribute in the CNS aqueous space as dictated by interstitial and cellular pH values. Our structure-activity analysis of 134 novel compounds considers primarily imidazole… CONTINUE READING
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Chapter 8. Anticholinesterase Agents

  • P. Taylor
  • The Pharmacological Basis of Therapeutics,
  • 2011
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