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Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1).
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2010 Nov 09; Vol. 2 (2), pp. 102-6. Date of Electronic Publication: 2010 Nov 09 (Print Publication: 2011). - Publication Year :
- 2010
-
Abstract
- Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at 0.3 mg/kg, 14 significantly reduced blood lymphocyte counts 24 h postdose and attenuated a delayed type hypersensitivity (DTH) response to antigen challenge.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 2
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24900287
- Full Text :
- https://doi.org/10.1021/ml100228m