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Bioorg Med Chem Lett. 2009 Apr 15;19(8):2315-9. doi: 10.1016/j.bmcl.2009.02.073. Epub 2009 Feb 23.

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

Author information

1
Department of Medicinal Chemistry, Praecis Pharmaceuticals Incorporated, Waltham, MA 02451, United States. ghotas.x.evindar@gsk.com

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) demonstrated potent and dose-responsive lymphopenia.

PMID:
19282175
DOI:
10.1016/j.bmcl.2009.02.073
[Indexed for MEDLINE]

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