| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371142 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Compounds containing 2-arybenzimidazole ring systems linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of structure–activity relationship studies led to the identification of compound 4c as a potent MCH-R1 antagonist (IC50 = 1 nM). This compound also has good metabolic stability, and favorable pharmacokinetic and brain penetration properties. However 4c was found to be potent inhibitor of the hERG potassium channel.
Graphical abstractThe synthesis and SAR of 2-arylbenzimidazoles as MCH-R1 antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chae Jo Lim, Nakjeong Kim, Eun Kyoung Lee, Byung Ho Lee, Kwang-Seok Oh, Sung-eun Yoo, Kyu Yang Yi,