| Literature DB >> 27055941 |
Junqing Guo1, Scott H Watterson2, Steven H Spergel2, James Kempson2, Charles M Langevine2, Ding Ren Shen2, Melissa Yarde2, Mary Ellen Cvijic2, Dana Banas2, Richard Liu2, Suzanne J Suchard2, Kathleen Gillooly2, Tracy Taylor2, Sandra Rex-Rabe2, David J Shuster2, Kim W McIntyre2, Georgia Cornelius2, Celia D'Arienzo2, Anthony Marino2, Praveen Balimane2, Luisa Salter-Cid2, Murray McKinnon2, Joel C Barrish2, Percy H Carter2, William J Pitts2, Jenny Xie2, Alaric J Dyckman2.
Abstract
The synthesis and structure-activity relationship (SAR) of a series of pyridyl-isoxazole based agonists of S1P1 are discussed. Compound 5b provided potent in vitro activity with selectivity, had an acceptable pharmacokinetic profile, and demonstrated efficacy in a dose dependent manner when administered orally in a rodent model of arthritis.Entities:
Keywords: FTY720; Fingolimod; Isoxazole; S1P(1); Sphingosine-1-phosphate; Sphingosine-1-phosphate 1
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Year: 2016 PMID： 27055941 DOI： 10.1016/j.bmcl.2016.03.105
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823