Design, synthesis and biological evaluation of fingolimod analogues containing diphenyl ether moiety.
- Author:
Gang LI
;
Weijuan HAN
;
Jing JIN
;
Xiaojian WANG
;
Qiong XIAO
;
Wanqi ZHOU
;
Dali YIN
;
Xiaoguang CHEN
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2014;49(6):896-904
- CountryChina
- Language:Chinese
-
Abstract:
A novel series of fingolimod analogues containing diphenyl ether moiety were designed and synthesized based on the modification of immunosuppressive agent fingolimod used in the treatment of multiple sclerosis. Compounds were evaluated in vivo for lymphopenic activity and heart rate affection. Most compounds showed moderate lymphopenic activity. It is worth noting that compounds 6c, 6d and 14c-14e showed considerable immunosuppressive activities comparable to fingolimod. And compound 14e had no effect on heart rate.
