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ID: ALA1137625
Journal: Bioorg Med Chem Lett
Title: Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.
Authors: Luci DK, Ghosh S, Smith CE, Qi J, Wang Y, Haertlein B, Parry TJ, Li J, Almond HR, Minor LK, Damiano BP, Kinney WA, Maryanoff BE, Lawson EC.
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.
CiteXplore: 17933531