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

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• 作者：Qinghua Meng ; Baowei Zhao ; Qiongfeng Xu ; Xuesong Xu ; Guanghui Deng ; Chengyong Li ; Linbo Luan ; Feng Ren ; Hailong Wang ; Heng Xu ; Yan Xu ; Haibo Zhang ; Jia-Ning Xiang ; John D. Elliott ; Taylor B. Guo ; Yonggang Zhao ; Wei Zhang ; Hongtao Lu ; Xichen Lin ; ^{Xichen.2.Lin@gsk.com}
• 关键词：Sphingosine-1-phosphate ; Agonist ; Lymphopenia ; Experimental autoimmune encephalomyelitis (EAE) ; SAR
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April, 2012
• 卷：22
• 期：8
• 页码：2794-2797
• 文件大小：1976 K

摘要

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 and has an excellent efficacy in mouse experimental autoimmune encephalomyelitis (EAE).