Synthesis and immunomodulating activity of new analogues of fingolimod

Five new immunomodulators 1a-1e by using a trans-4-alkyl-substituted cyclohexane to replace the flexible C8 alkyl chain of Fingolimod were synthesized. For in-vitro test, the compounds were dissolved in DMSO as a stock solution and diluted to a desired concentration with RPMI 1640 nutrient solution. For in-vivo test, the compounds were prepared in pathogen-free saline containing 0.5% DMSO. These new immunomodulators displayed more potent immunoinhibitory activities in vitro and moderate immunomodulating activities in vivo. They show therapeutic effects on DNFB-induced DTH reaction and inhibitory effects on the antigen-specific T-cell proliferation. Five new immunomodulators 1a-1e were synthesized by using a trans-4-alkyl-substituted cyclohexane to replace the flexible C8 alkyl chain of fingolimod. They show therapeutic effects on the DNFB-induced DTH reaction and inhibitory effects on antigen-specific T-cell proliferation.