Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
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ABSTRACT:
SUBMITTER: Ma B
PROVIDER: S-EPMC2843818 | biostudies-literature | 2010 Apr
REPOSITORIES: biostudies-literature
Publications
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Ma Bin B Guckian Kevin M KM Lin Edward Yin-Shiang EY Lee Wen-Cherng WC Scott Daniel D Kumaravel Gnanasambandam G Macdonald Timothy L TL Lynch Kevin R KR Black Cheryl C Chollate Sowmya S Hahm Kyungmin K Hetu Gregg G Jin Ping P Luo Yi Y Rohde Ellen E Rossomando Anthony A Scannevin Robert R Wang Joy J Yang Chunhua C
Bioorganic & medicinal chemistry letters 20100206 7
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. ...[more]
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