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Design and Synthesis of Selective and Potent Orally Active S1P5 Agonists

Kumar Dev, Kumlesh and Bouhelal, Rochdi and Barske, Carmen and Guerini, Danilo and Gasparini, Fabrizio and Mir, Anis Khusro and Orain, David and Osinde, Maribel and Picard, Anne and Dubois, Celine and Tasdelen, Engin and Haessig, Samuel and Mattes, Henri (2010) Design and Synthesis of Selective and Potent Orally Active S1P5 Agonists. ChemMedChem, 5 (10). pp. 1693-1696. ISSN 1860-7179


Putting the brakes on demyelination: Fingolimod (FTY720) was recently shown to significantly decrease relapse rates in patients with multiple sclerosis. This drug attenuates the trafficking of harmful T-cells entering the brain by regulating sphingosine-1-phosphate (S1P) receptors. We designed, synthesized, evaluated 2H-phthalazin-1-one derivatives (e.g., 1 L) as selective S1P5 receptor agonists; these compounds are highly potent and selective, with good PK properties, and significant activity in oligodendrocytes.

Item Type: Article
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Additional Information: archiving not allowed on institutional repository
Keywords: FTY720; sphingosine; S1P5 agonists; oligodendrocytes; myelination
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Date Deposited: 13 Oct 2015 13:16
Last Modified: 13 Oct 2015 13:16


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