Title of article :
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: Synthesis, SAR, and in vivo assessment
Author/Authors :
Diane K. Luci، نويسنده , , Shyamali Ghosh، نويسنده , , Charles E. Smith، نويسنده , , Jenson Qi، نويسنده , , Yuanping Wang، نويسنده , , Barbara Haertlein، نويسنده , , Tom J. Parry، نويسنده , , Jian Li، نويسنده , , Harold R. Almond Jr.، نويسنده , , Lisa K. Minor، نويسنده , , Bruce P. Damiano، نويسنده , , William A. Kinney، نويسنده , , Bruce E. Maryanoff، نويسنده , , Edward C. Lawson، نويسنده ,
Abstract :
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.
Keywords :
piperidine , Urotensin , Ear flush , Antagonist
