Toshiyuki Kohara

Design, synthesis, and structure-activity relationships of 2-substituted-2-amino-1,3-propanediols: Discovery of a novel immunosuppressant, FTY720

FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol hydrochloride), a novel synthetic immunosuppressant led by modification of ISP-I (myriocin, thermozymocidin) displayed potent immunosuppressive activity both in vitro and in vivo.

Synthesis and biological evaluation of 2,2-disubstituted 2-aminoethanols: analogues of FTY720

Desymmerization of symmetric FTY720 by substitution of different alkyl groups for one of the prochiral hydroxymethyl groups was performed. The size of the alkyl groups and the absolute configuration at quaternary carbon were important on immunosuppressive activity.