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  • Title: Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.
    Author: Kobayashi K, Uchiyama M, Ito H, Takahashi H, Yoshizumi T, Sakoh H, Nagatomi Y, Asai M, Miyazoe H, Tsujita T, Hirayama M, Ozaki S, Tani T, Ishii Y, Ohta H, Okamoto O.
    Journal: Bioorg Med Chem Lett; 2009 Jul 01; 19(13):3627-31. PubMed ID: 19447610.
    Abstract:
    The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1H-pyrazol-3-yl]methyl}-3-fluorocyclopentanamine, which exhibits high intrinsic potency and selectivity against other opioid receptors and hERG potassium channel.
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