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

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

  • J Med Chem. 2005 Oct 6;48(20):6169-73. doi: 10.1021/jm0503244.
Zhen Li 1,  Weirong Chen,  Jeffrey J Hale,  Christopher L Lynch,  Sander G Mills,  Richard Hajdu,  Carol Ann Keohane,  Mark J Rosenbach,  James A Milligan,  Gan-Ju Shei,  Gary Chrebet,  Stephen A Parent,  James Bergstrom,  Deborah Card,  Michael Forrest,  Elizabeth J Quackenbush,  L Alexandra Wickham,  Hugo Vargas,  Rose M Evans,  Hugh Rosen,  Suzanne Mandala
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratory, Rahway, New Jersey 07065, USA. zhen_li@merck.com
PMID: 16190743 DOI: 10.1021/jm0503244
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.

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