4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

@article{Mistry20164Phenylpyridin2oneDA,
  title={4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.},
  author={Shailesh N Mistry and Manuela J{\"o}rg and Herman D. Lim and Natalie B. Vinh and Patrick M. Sexton and Ben Capuano and Arthur Christopoulos and J Robert Lane and Peter J. Scammells},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 1},
  pages={388-409}
}
Positive allosteric modulators (PAMs) of the M1 muscarinic acetylcholine receptor (M1 mAChR) are a promising strategy for the treatment of the cognitive deficits associated with diseases including Alzheimer's and schizophrenia. Herein, we report the design, synthesis, and characterization of a novel family of M1 mAChR PAMs. The most active compounds of the 4-phenylpyridin-2-one series exhibited comparable binding affinity to the reference compound, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline… CONTINUE READING