S1P 受体介导的 FTY720 磷酸盐类似物的活性。

S1P receptor mediated activity of FTY720 phosphate mimics.

机构信息

Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.

出版信息

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1485-7. doi: 10.1016/j.bmcl.2010.01.118. Epub 2010 Jan 28.

DOI:10.1016/j.bmcl.2010.01.118

PMID:20153186

Abstract

Various carboxylic acids, phosphonic acids, sulfonic acids, tetrazoles as well as sulfonylhydantoins were prepared as phosphate mimics of the chiral aminophosphate 1-P to act as agonists on the S1P(1) receptor. It was found that amino phosphonates and amino carboxylates are potent S1P(1) binders. beta-Amino acid 11 could be shown to reversibly reduce blood lymphocyte counts in rats after po administration.

摘要

各种羧酸、膦酸、磺酸、四唑以及磺酰基脲被制备为手性氨基磷酸 1-P 的磷酸盐类似物，用作 S1P(1)受体的激动剂。结果发现，氨基膦酸酯和氨基羧酸酯是有效的 S1P(1)结合物。β-氨基酸 11 经 po 给药后可在大鼠体内可逆地降低血液淋巴细胞计数。