- Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Bioorganic & medicinal chemistry letters (2010-03-02)
Bin Ma, Kevin M Guckian, Edward Yin-Shiang Lin, Wen-Cherng Lee, Daniel Scott, Gnanasambandam Kumaravel, Timothy L Macdonald, Kevin R Lynch, Cheryl Black, Sowmya Chollate, Kyungmin Hahm, Gregg Hetu, Ping Jin, Yi Luo, Ellen Rohde, Anthony Rossomando, Robert Scannevin, Joy Wang, Chunhua Yang
PMID20188554
RÉSUMÉ
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.
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