Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors |
| |
| 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 |
| |
| Affiliation: | 1. Research Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea;2. Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea |
| |
| 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: | Heart failure G-protein-coupled receptor kinase-2 (GRK-2) GRK-5 Benzoxazole |
| 本文献已被 ScienceDirect 等数据库收录！ |
