188928-06-5Relevant academic research and scientific papers
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold
He, Xinhua,Wang, Lili,Zheng, Zhibing,Xiao, Junhai,Zhong, Wu,Li, Song
, p. 553 - 557 (2012/03/11)
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-P, at a dose of 10 mg/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.
