2,5-二取代吡咯烷羧酸酯作为强效的口服活性鞘氨醇-1-磷酸（S1P）受体激动剂。
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
作者信息
Colandrea Vincent J, Legiec Irene E, Huo Pei, Yan Lin, Hale Jeffrey J, Mills Sander G, Bergstrom James, Card Deborah, Chebret Gary, Hajdu Richard, Keohane Carol Ann, Milligan James A, Rosenbach Mark J, Shei Gan-Ju, Mandala Suzanne M
机构信息
Department of Medical Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jun 1;16(11):2905-8. doi: 10.1016/j.bmcl.2006.03.038. Epub 2006 Mar 31.
PMID:16580205
Abstract
A series of 2,5-cis-disubstituted pyrrolidines were synthesized and evaluated as S1P receptor agonists. Compounds 15-21 were identified with good selectivity over S1P3 which lowered circulating lymphocytes after oral administration in mice.
摘要
合成了一系列2,5-顺式二取代吡咯烷，并将其作为鞘氨醇-1-磷酸（S1P）受体激动剂进行评估。鉴定出化合物15 - 21对S1P3具有良好的选择性，口服给药后可降低小鼠循环淋巴细胞水平。
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