Details

Autor(en) / Beteiligte

• Ma, Bin
• Guckian, Kevin M
• Liu, Xiao-gao
• Yang, Chunhua
• Li, Bing
• Scannevin, Robert
• Mingueneau, Michaël
• Drouillard, Annabelle
• Walzer, Thierry

Titel

Novel Potent Selective Orally Active S1P5 Receptor Antagonists

Ist Teil von

• ACS medicinal chemistry letters, 2021-03, Vol.12 (3), p.351-355

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2021

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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.