94308-71-1Relevant articles and documents
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment
Luci, Diane K.,Ghosh, Shyamali,Smith, Charles E.,Qi, Jenson,Wang, Yuanping,Haertlein, Barbara,Parry, Tom J.,Li, Jian,Almond Jr., Harold R.,Minor, Lisa K.,Damiano, Bruce P.,Kinney, William A.,Maryanoff, Bruce E.,Lawson, Edward C.
, p. 6489 - 6492 (2008/03/13)
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.
