Structure-activity relationships for inhibition of human cholinesterases by alkyl amide phenothiazine derivatives.

@article{Darvesh2005StructureactivityRF,
  title={Structure-activity relationships for inhibition of human cholinesterases by alkyl amide phenothiazine derivatives.},
  author={Sultan Darvesh and Robert S McDonald and Andrea Penwell and Sarah K. Conrad and Katherine V Darvesh and Diane Mataija and Geraldine T Gomez and Angela Caines and Ryan Walsh and Earl Martin},
  journal={Bioorganic & medicinal chemistry},
  year={2005},
  volume={13 1},
  pages={211-22}
}
Several lines of evidence indicate that inhibition of butyrylcholinesterase (BuChE) is important in the treatment of certain dementias. Further testing of this concept requires inhibitors that are both BuChE-selective and robust. N-alkyl derivatives (2, 3, 4) of phenothiazine (1) have previously been found to inhibit only BuChE in a mechanism involving pi-pi interaction between the phenothiazine tricyclic ring system and aromatic residues in the active site gorge. To explore features of… CONTINUE READING

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