- Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.
Bioorganic & medicinal chemistry letters (2007-10-16)
Diane K Luci, Shyamali Ghosh, Charles E Smith, Jenson Qi, Yuanping Wang, Barbara Haertlein, Tom J Parry, Jian Li, Harold R Almond, Lisa K Minor, Bruce P Damiano, William A Kinney, Bruce E Maryanoff, Edward C Lawson
PMID17933531
摘要
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.
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