Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.

@article{Luci2007PhenylpiperidinebenzoxazinonesAU,
  title={Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.},
  author={Diane K Luci and Shyamali Ghosh and C. I. Edvard Smith and Jenson Qi and Yuanping Wang and Barbara J Haertlein and Tom J. Parry and Jian Li and Harold R Almond and Lisa K Minor and Bruce P Damiano and William A. Kinney and Bruce E Maryanoff and Edward C Lawson},
  journal={Bioorganic & medicinal chemistry letters},
  year={2007},
  volume={17 23},
  pages={6489-92}
}
Various 4-phenylpiperidine-benzoxazin-3-ones were synthesized and biologically evaluated as urotensin-II (U-II) receptor antagonists. Compound 12i was identified from in vitro evaluation as a low nanomolar antagonist against both rat and human U-II receptors. This compound showed in vivo efficacy in reversing the ear-flush response induced by U-II in rats.