| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373758 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A structure–activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over binding affinity for hERG and other opioid receptors.
Graphical abstractOptimization of benzimidazole series as ORL1 antagonists is reported. Compound 7h exhibited potent ORL1 activity with high selectivity over binding affinity for hERG.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kensuke Kobayashi, Tetsuya Kato, Izumi Yamamoto, Atsushi Shimizu, Sayaka Mizutani, Masanori Asai, Hiroshi Kawamoto, Satoru Ito, Takashi Yoshizumi, Mioko Hirayama, Satoshi Ozaki, Hisashi Ohta, Osamu Okamoto,