2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists

Vincent J. Colandrea,Irene E. Legiec,Pei Huo,Lin Yan,Jeffrey J. Hale,Sander G. Mills,James Bergstrom,Deborah Card,Gary Chebret,Richard Hajdu,Carol Ann Keohane,James A. Milligan,Mark J. Rosenbach,Gan-Ju Shei,Suzanne M. Mandala

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

A series of 2-aryl(pyrrolidine-5-yl)acetic acids (e.g., 21) were synthesized and evaluated as S1P receptor agonists. Compounds 15–21 were identified with good selectivity over S1P3 and found to lower peripheral lymphocytes after oral administration in mice.

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关键词

Pyrrolidines,Oxadiazole,S1P receptor,Immunosuppressants

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