A series of oxazolidin-2-one-4-carboxylic amide compounds (1a–f) were designed and synthesized as the non-phosphate S1P1 receptor agonists. The single crystal of 1e was prepared and solved to elucidate the structure of 1a–f. EC50 of 1a–d were about 1.1–3.6 μM in S1P1 Redistribution® assay, and their cytotoxicity was 8–40-fold lower than FTY720. Though its S1P1 agonist activities in vitro were about 1000-folds weaker than (S)-FTY720- ...