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2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists |
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| Authors: | Colandrea Vincent J Legiec Irene E Huo Pei Yan Lin Hale Jeffrey J Mills Sander G Bergstrom James Card Deborah Chebret Gary Hajdu Richard Keohane Carol Ann Milligan James A Rosenbach Mark J Shei Gan-Ju Mandala Suzanne M |
| Affiliation: | Department of Medical Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. vince_colandrea@merck.com |
| 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. |
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