发现噻二唑酰胺是有效的、能够避免与鞘氨醇-1-磷酸 1（S1P1）受体结合的鞘氨醇-1-磷酸 1（S1P1）受体激动剂。
Discovery of thiadiazole amides as potent, S1P₃-sparing agonists of sphingosine-1-phosphate 1 (S1P₁) receptor.
机构信息
GlaxoSmithKline Pharmaceuticals, R&D China, 898 Halei Road, Zhangjiang Hi-Tech Park, Pudong, Shanghai 201023, China.
出版信息
Bioorg Med Chem Lett. 2012 Apr 1;22(7):2456-9. doi: 10.1016/j.bmcl.2012.02.016. Epub 2012 Feb 15.
PMID:22386243
Abstract
High-throughput screening of GSK compound collection led to the discovery of a novel series of thiadiazole amides as potent and S1P(3)-sparing sphingosine-1-phosphate 1 (S1P(1)) receptor agonists. Synthesis, structure and activity relationship, selectivity, and some developability properties are described.
摘要
高通量筛选 GSK 化合物库发现了一系列新型噻二唑酰胺类化合物，它们是有效的且能避免 S1P(3)的鞘氨醇-1-磷酸 1（S1P(1)）受体激动剂。本文描述了它们的合成、结构与活性关系、选择性以及一些可开发性特征。
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