Novel 2,4-Disubstituted Pyrimidines as Potent, Selective, and Cell-Permeable Inhibitors of Neuronal Nitric Oxide Synthase

@inproceedings{Mukherjee2015Novel2P,
  title={Novel 2,4-Disubstituted Pyrimidines
as Potent, Selective, and Cell-Permeable Inhibitors of Neuronal Nitric
Oxide Synthase},
  author={Paramita Mukherjee and Huiying Li and Irina F Sevrioukova and Georges Chreifi and P Martasek and Linda J. Roman and Thomas L Poulos and Richard B Silverman},
  booktitle={Journal of medicinal chemistry},
  year={2015}
}
Selective inhibition of neuronal nitric oxide synthase (nNOS) is an important therapeutic approach to target neurodegenerative disorders. However, the majority of the nNOS inhibitors developed are arginine mimetics and, therefore, suffer from poor bioavailability. We designed a novel strategy to combine a more pharmacokinetically favorable 2-imidazolylpyrimidine head with promising structural components from previous inhibitors. In conjunction with extensive structure-activity studies, several… CONTINUE READING

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