2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors

A series of 2-aryl(pyrrolidin-4-yl)acetic acids were synthesized and their biological activities were evaluated as agonists of S1P receptors. These analogs were able to induce lowering of lymphocyte counts in the peripheral blood of mice and were found to have good overall pharmacokinetic properties in rat.

Graphical abstractA series of 2-aryl(pyrrolidine-4-yl)acetic acids (e.g., 22g) were synthesized and evaluated as S1P receptor agonists and were found to lower peripheral lymphocyte counts in mice and to have good overall pharmacokinetic properties in rat.Figure optionsDownload full-size imageDownload as PowerPoint slide