Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.

作者: Qinghua Meng , Baowei Zhao , Qiongfeng Xu , Xuesong Xu , Guanghui Deng

DOI: 10.1016/J.BMCL.2012.02.083

关键词: ChemistrySphingosine-1-phosphateReceptorBiochemistryPeripheral blood lymphocyteAgonistPharmacologyS1p1 receptorIn vivoIndole testExperimental autoimmune encephalomyelitis

摘要: Abstract Novel indole-propionic acid derivatives were developed as sphingosine-1-phosphate (S1P) receptor agonists through a systematic SAR study. The optimized and S1P3 selective S1P1 agonist 9f induced peripheral blood lymphocyte reduction in vivo has an excellent efficacy mouse experimental autoimmune encephalomyelitis (EAE).

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