具有 N-肉桂基-β-丙氨酸部分的鞘氨醇-1-磷酸受体激动剂的构效关系研究。
Structure-activity relationship studies of sphingosine-1-phosphate receptor agonists with N-cinnamyl-β-alanine moiety.
机构信息
Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, Mishima, Osaka 618-8585, Japan.
出版信息
Bioorg Med Chem Lett. 2011 Mar 1;21(5):1390-3. doi: 10.1016/j.bmcl.2011.01.029. Epub 2011 Jan 11.
PMID:21295477
Abstract
Structure-activity relationship of sphingosine-1-phosphate receptor agonist was examined. In terms of reducing the flexibility of molecule, hit compound 1 was modified to improve S1P(1) agonistic activity as well as selectivity over S1P(3) agonistic activity. Novel S1P agonists with cinnamyl scaffold or 1,2,5,6-tetrahydropyridine scaffold were identified.
摘要
我们研究了神经鞘氨醇-1-磷酸受体激动剂的构效关系。为了降低分子的灵活性，对先导化合物 1 进行了修饰，以提高其对 S1P（1）的激动活性，并提高对 S1P（3）的激动活性的选择性。鉴定出具有肉桂基骨架或 1,2,5,6-四氢吡啶骨架的新型 S1P 激动剂。
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