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Bioorg Med Chem Lett. 2010 Apr 1;20(7):2264-9. doi: 10.1016/j.bmcl.2010.02.006. Epub 2010 Feb 6.

Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.

Author information

1
BiogenIdec Inc., 14 Cambridge Center, Cambridge, MA 02142, USA. bin.ma@biogenidec.com

Abstract

Modifying FTY720, an immunosuppressant modulator, led to a new series of well phosphorylated tetralin analogs as potent S1P1 receptor agonists. The stereochemistry effect of tetralin ring was probed, and (-)-(R)-2-amino-2-((S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propan-1-ol was identified as a good SphK2 substrate and potent S1P1 agonist with good oral bioavailability.

PMID:
20188554
PMCID:
PMC2843818
DOI:
10.1016/j.bmcl.2010.02.006
[Indexed for MEDLINE]
Free PMC Article

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