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Bioorg Med Chem Lett. 2013 Jan 15;23(2):472-5. doi: 10.1016/j.bmcl.2012.11.053. Epub 2012 Nov 27.

Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.

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Department of Medicinal Chemistry, Praecis Pharmaceuticals Incorporated (Currently GlaxoSmithKline), 830 Winter Street, Waltham, MA 02451, USA.


In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group as a replacement to previously reported lead phosphates. This has led to the discovery of potent and selective direct agonists with moderate to substantial in vivo lymphopenia. The previously reported selectivity enhancing moiety (SEM) and selectivity enhancing orientation (SEO) in the phenylamide and phenylimidazole scaffolds were crucial to obtaining selectivity for S1P receptor subtype 1 over 3.

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