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, 19 (2), 369-72

Synthesis and Evaluation of Alkoxy-Phenylamides and Alkoxy-Phenylimidazoles as Potent sphingosine-1-phosphate Receptor subtype-1 Agonists

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Synthesis and Evaluation of Alkoxy-Phenylamides and Alkoxy-Phenylimidazoles as Potent sphingosine-1-phosphate Receptor subtype-1 Agonists

Ghotas Evindar et al. Bioorg Med Chem Lett.

Abstract

In the design of potent and selective sphingosine-1-phosphate receptor agonists, we were able to identify two series of molecules based on phenylamide and phenylimidazole analogs of FTY-720. Several designed molecules in these scaffolds have demonstrated selectivity for S1P receptor subtype 1 versus 3 and excellent in vivo activity in mouse. Two molecules PPI-4621 (4b) and PPI-4691 (10a), demonstrated dose responsive lymphopenia, when administered orally.

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