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. 2014 Oct 15;24(20):4807-11.
doi: 10.1016/j.bmcl.2014.09.003. Epub 2014 Sep 6.

Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists

Joshua C Horan  1 , Sulagna Sanyal  2 , Younggi Choi  2 , Melissa Hill-Drzewi  2 , Lori Patnaude  3 , Shawn Anderson  3 , Steve Fogal  3 , Can Mao  2 , Brian N Cook  2 , Kristina Gueneva-Boucheva  2 , Michael B Fisher  2 , Eugene Hickey  2 , Edward Pack  2 , Lynne C Bannen  4 , Diva S Chan  4 , Morrison B Mac  4 , Stephanie M Ng  4 , Yong Wang  4 , Wei Xu  4 , Louise K Modis  3 , René M Lemieux  2
Affiliations

Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists

Joshua C Horan et al. Bioorg Med Chem Lett. .

Abstract

The discovery of a new series of selective S1P1 agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR studies showed that 10d was converted to the active phosphate metabolite 29 in vivo. Oral administration of compound 10d to rats was shown to induce lymphopenia at 3 mg/kg.

Keywords: Agonist; Lymphopenia; Prodrug; S1P1; S1P3.

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