Synthesis and evaluation of arylalkoxy-and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 …

…, E Doyle, J Lorusso, N Taghizadeh, K Halley…

Index: Evindar, Ghotas; Satz, Alexander L.; Bernier, Sylvie G.; Kavarana, Malcolm J.; Doyle, Elisabeth; Lorusso, Jeanine; Taghizadeh, Nazbeh; Halley, Keith; Hutchings, Amy; Kelley, Michael S.; Wright, Albion D.; Saha, Ashis K.; Hannig, Gerhard; Morgan, Barry A.; Westlin, William F. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 8 p. 2315 - 2319

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Citation Number: 10

Abstract

In pursuit of potent and selective sphingosine-1-phosphate receptor agonists, we have utilized previously reported phenylamide and phenylimidazole scaffolds to explore extensive side-chain modifications to generate new molecular entities. A number of designed molecules demonstrate good selectivity and excellent in vitro and in vivo potency in both mouse and rat models. Oral administration of the lead molecule 11c (PPI-4667) ...