Title of article :
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists
Author/Authors :
Vincent J. Colandrea، نويسنده , , Irene E. Legiec، نويسنده , , Pei Huo، نويسنده , , Lin Yan، نويسنده , , Jeffrey J. Hale، نويسنده , , Sander G. Mills، نويسنده , , James Bergstrom، نويسنده , , Deborah Card، نويسنده , , Gary Chebret، نويسنده , , Richard Hajdu، نويسنده , , Carol Ann Keohane، نويسنده , , James A. Milligan، نويسنده , , Mark J. Rosenbach، نويسنده , , Gan-Ju Shei، نويسنده , , Suzanne M. Mandala، نويسنده ,
Abstract :
A series of 2,5-cis-disubstituted pyrrolidines were synthesized and evaluated as S1P receptor agonists. Compounds 15–21 were identified with good selectivity over S1P3 which lowered circulating lymphocytes after oral administration in mice.
Keywords :
S1P receptor , Oxadiazole , Pyrrolidines , Immunosuppressants