|
|||||
|
|
2,3-Diphenylpropionic acids as potent VLA-4 antagonists |
|
| Authors: | Hoshina Yoichiro Ikegami Satoru Okuyama Akihiko Fukui Hideto Inoguchi Kiyoshi Maruyama Tatsuya Fujimoto Kyoko Matsumura Yuzuru Aoyama Akinori Harada Tatsuhiro Tanaka Hiroshi Nakamura Tsutomu |
| Affiliation: | Central Research Laboratories, Kaken Pharmaceutical Co. Ltd, 14 Shinomiya-minamikawara, Yamashina, Kyoto 607-8042, Japan. |
| Abstract: | The discovery and SAR of 2,3-diphenylpropionic acid derivatives as highly potent VLA-4 antagonists are described. One representative compound, 9cc has inhibited intercellular adhesion by a VCAM-1/VLA-4 interaction with an IC(50) of 1.7 nM, and has good pharmacokinetics and oral bioavailability. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |