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Bioorg Med Chem Lett. 2012 Jan 1;22(1):553-7. doi: 10.1016/j.bmcl.2011.10.088. Epub 2011 Nov 6.

Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.

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Beijing Institute of Pharmacology & Toxicology, No.27 Taiping Road, Beijing 100850, PR China.


A series of oxazolidin-2-one-4-carboxylic amide compounds (1a-f) were designed and synthesized as the non-phosphate S1P(1) receptor agonists. The single crystal of 1e was prepared and solved to elucidate the structure of 1a-f. EC(50) of 1a-d were about 1.1-3.6 μM in S1P(1) Redistribution® assay, and their cytotoxicity was 8-40-fold lower than FTY720. Though its S1P(1) agonist activities in vitro were about 1000-folds weaker than (S)-FTY720-P, at a dose of 10mg/Kg, the immunosuppressive effects of 1a were comparable to FTY720. So oxazolidin-2-one-4-carboxylic amide derivatives were found as potential immunomodulator, compound 1a could be considered as a lead compound, rational modifications of 1a are anticipated using medicinal chemistry techniques and molecular modeling to obtain analogs with higher affinity and better clinical therapeutic properties.

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