Author/Authors :
Yoichiro Hoshina، نويسنده , , Satoru Ikegami، نويسنده , , Akihiko Okuyama، نويسنده , , Hideto Fukui، نويسنده , , Kiyoshi Inoguchi، نويسنده , , Tatsuya Maruyama، نويسنده , , Kyoko Fujimoto، نويسنده , , Yuzuru Matsumura، نويسنده , , Akinori Aoyama، نويسنده , , Tatsuhiro Harada، نويسنده , , Hiroshi Tanaka ، نويسنده , , Tsutomu Nakamura، نويسنده ,
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 IC50 of 1.7 nM, and has good pharmacokinetics and oral bioavailability.
Keywords :
2 , 3-Diphenylpropionic acid , VLA-4 , VCAM-1
