Novel Potent Selective Orally Active S1P5 Receptor Antagonists

S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we de...

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Bibliographic Details
Published in:ACS medicinal chemistry letters 2021-03, Vol.12 (3), p.351-355
Main Authors: Ma, Bin, Guckian, Kevin M, Liu, Xiao-gao, Yang, Chunhua, Li, Bing, Scannevin, Robert, Mingueneau, Michaël, Drouillard, Annabelle, Walzer, Thierry
Format: Article
Language:English
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Summary:S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.0c00631