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J Med Chem. 2005 Oct 6;48(20):6169-73.

Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.

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1
Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, New Jersey 07065, USA. zhen_li@merck.com

Abstract

A class of 3,5-diphenyl-1,2,4-oxadiazole based compounds have been identified as potent sphingosine-1-phosphate-1 (S1P1) receptor agonists with minimal affinity for the S1P2 and S1P3 receptor subtypes. Analogue 26 (S1P1 IC50 = 0.6 nM) has an excellent pharmacokinetics profile in the rat and dog and is efficacious in a rat skin transplant model, indicating that S1P3 receptor agonism is not a component of immunosuppressive efficacy.

PMID:
16190743
DOI:
10.1021/jm0503244
[Indexed for MEDLINE]
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