Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists
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DOI：
10.1016/j.bmcl.2012.02.083
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发表时间：
2012-04-15
影响因子：
2.7
通讯作者：
Lin, Xichen
中科院分区：
文献类型：
--
作者：
Meng, Qinghua;Zhao, Baowei;Lin, Xichen
通过系统的 SAR 研究，开发了新型吲哚丙酸衍生物作为 1-磷酸鞘氨醇 (S1P) 受体激动剂。优化的S1P(3)选择性S1P(1)激动剂9f可诱导体内外周血淋巴细胞减少，对小鼠实验性自身免疫性脑脊髓炎(EAE)具有优异的疗效。 (C) 2012 Elsevier Ltd. 保留所有权利。
Novel indole-propionic acid derivatives were developed as sphingosine-1-phosphate (S1P) receptor agonists through a systematic SAR study. The optimized and S1P(3) selective S1P(1) agonist 9f induced peripheral blood lymphocyte reduction in vivo and has an excellent efficacy in mouse experimental autoimmune encephalomyelitis (EAE). (C) 2012 Elsevier Ltd. All rights reserved.