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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
6489
To page
6492
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798830
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