LI Gang, HAN Wei-juan, JIN Jing, WANG Xiao-jian, XIAO Qiong, ZHOU Wan-qi, YIN Da-li, CHEN Xiao-guang. Design, synthesis and biological evaluation of fingolimod analogues containing diphenyl ether moietyJ. Acta Pharmaceutica Sinica, 2014,49(6): 896-904.
Citation: LI Gang, HAN Wei-juan, JIN Jing, WANG Xiao-jian, XIAO Qiong, ZHOU Wan-qi, YIN Da-li, CHEN Xiao-guang. Design, synthesis and biological evaluation of fingolimod analogues containing diphenyl ether moietyJ. Acta Pharmaceutica Sinica, 2014,49(6): 896-904.

Design, synthesis and biological evaluation of fingolimod analogues containing diphenyl ether moiety

  • 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.Mostcompounds 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 noeffect on heart rate.
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