Discovery of thiadiazole amides as potent, S1P 3-sparing agonists of sphingosine-1-phosphate 1 (S1P 1) receptor

…, C Li, Y Wang, F Han, T Yang, F Ren, JN Xiang…

Index: Xu, Heng; Zhang, Haibo; Luan, Linbo; Xu, Yan; Li, Chengyong; Wang, Yonghui; Han, Fangbin; Yang, Ting; Ren, Feng; Xiang, Jia-Ning; Elliott, John D.; Zhao, Yonggang; Guo, Taylor B.; Lu, Hongtao; Zhang, Wei; Hirst, David; Lindon, Matthew; Lin, Xichen Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2456 - 2459

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Abstract

High-throughput screening of GSK compound collection led to the discovery of a novel series of thiadiazole amides as potent and S1P3-sparing sphingosine-1-phosphate 1 (S1P1) receptor agonists. Synthesis, structure and activity relationship, selectivity, and some developability properties are described.