Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593302 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
G-protein-coupled receptor kinase (GRK)-2 and -5 are emerging therapeutic targets for the treatment of cardiovascular disease. In our efforts to discover novel small molecules to inhibit GRK-2 and -5, a class of compound based on 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine was identified as a novel hit by high throughput screening campaign. Structural modification of parent benzoxazole scaffolds by introducing substituents on phenyl displayed potent inhibitory activities toward GRK-2 and -5.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sung Yun Cho, Byung Ho Lee, Heejung Jung, Chang Soo Yun, Jae Du Ha, Hyoung Rae Kim, Chong Hak Chae, Jeong Hyun Lee, Ho Won Seo, Kwang-Seok Oh,