Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.

@article{Kono2013SynthesisSS,
  title={Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.},
  author={Mitsunori Kono and Takahiro Matsumoto and Toru Kawamura and Atsushi Nishimura and Yoshihiro Kiyota and Hideyuki Oki and Junichi Miyazaki and Shigeru Igaki and Craig A. Behnke and Masato Shimojo and Masakuni Kori},
  journal={Bioorganic & medicinal chemistry},
  year={2013},
  volume={21 1},
  pages={
          28-41
        }
}
A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the lead compound 3 to improve its DMPK profile as well as in vitro potency. We identified the thiazole compound 60j with potent inhibitory activity, high brain permeability, and good bioavailability. Compound 60j showed a potent and dose-dependent… CONTINUE READING
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