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Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists. 2009
Kensuke Kobayashi, and
Minaho Uchiyama, and
Hirokatsu Ito, and
Hirobumi Takahashi, and
Takashi Yoshizumi, and
Hiroki Sakoh, and
Yasushi Nagatomi, and
Masanori Asai, and
Hiroshi Miyazoe, and
Tomohiro Tsujita, and
Mioko Hirayama, and
Satoshi Ozaki, and
Takeshi Tani, and
Yasuyuki Ishii, and
Hisashi Ohta, and
Osamu Okamoto
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan.
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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