Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.

@article{Markwalder2017IdentificationAO,
  title={Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.},
  author={Jay A. Markwalder and Steven P. Seitz and Yuval Blat and Lisa Elkin and John T. Hunt and Jonathan G. Pabalan and Maria N. Jure-Kunkel and Gregory D. Vite and Kelly Covello},
  journal={Bioorganic & medicinal chemistry letters},
  year={2017},
  volume={27 3},
  pages={582-585}
}
The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.