|
|||||
|
|
Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists |
|
| Authors: | Kensuke Kobayashi 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 |
| Institution: | Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan |
| 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. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |