ACS Medicinal Chemistry Letters (2021)
Update date:2022-09-26
Topics:
Ma, Bin
Guckian, Kevin M.
Liu, Xiao-Gao
Yang, Chunhua
Li, Bing
Scannevin, Robert
Mingueneau, Micha?l
Drouillard, Annabelle
Walzer, Thierry
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.
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