2. Academic Validation
  3. Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists

Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists

  • Bioorg Med Chem Lett. 2009 Jul 1;19(13):3627-31. doi: 10.1016/j.bmcl.2009.04.116.
Kensuke Kobayashi 1,  Minaho Uchiyama,  Hirokatsu Ito,  Hirobumi Takahashi,  Takashi Yoshizumi,  Hiroki Sakoh,  Yasushi Nagatomi,  Masanori Asai,  Hiroshi Miyazoe,  Tomohiro Tsujita,  Mioko Hirayama,  Satoshi Ozaki,  Takeshi Tani,  Yasuyuki Ishii,  Hisashi Ohta,  Osamu Okamoto
Affiliations

Affiliation

  • 1 Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan.
PMID: 19447610 DOI: 10.1016/j.bmcl.2009.04.116
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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