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Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Apr 01; Vol. 20 (7), pp. 2264-9. Date of Electronic Publication: 2010 Feb 06. - Publication Year :
- 2010
-
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.<br /> (2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Crystallography, X-Ray
Immunosuppressive Agents chemistry
Immunosuppressive Agents metabolism
Immunosuppressive Agents pharmacokinetics
Lymphopenia chemically induced
Mice
Models, Molecular
Multiple Sclerosis drug therapy
Phosphorylation
Phosphotransferases (Alcohol Group Acceptor) metabolism
Prodrugs chemistry
Prodrugs metabolism
Prodrugs pharmacokinetics
Structure-Activity Relationship
Tetrahydronaphthalenes chemistry
Tetrahydronaphthalenes metabolism
Tetrahydronaphthalenes pharmacokinetics
Immunosuppressive Agents pharmacology
Prodrugs pharmacology
Receptors, Lysosphingolipid agonists
Receptors, Lysosphingolipid metabolism
Tetrahydronaphthalenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20188554
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.02.006