The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3495-9. doi: 10.1016/j.bmcl.2004.04.069.

Authors

Jeffrey J Hale¹, George Doherty, Leslie Toth, Zhen Li, Sander G Mills, Richard Hajdu, Carol Ann Keohane, Mark Rosenbach, James Milligan, Gan-Ju Shei, Gary Chrebet, James Bergstrom, Deborah Card, Hugh Rosen, Suzanne Mandala

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. [email protected]

PMID: 15177460
DOI: 10.1016/j.bmcl.2004.04.069

Abstract

3-(N-Alkyl)aminopropylphosphonic acids are potent agonists of four of the five known sphingosine-1-phosphate (S1P) receptor subtypes.

MeSH terms

Animals
CHO Cells
Cricetinae
Humans
Inhibitory Concentration 50
Ligands
Organophosphonates / chemical synthesis
Organophosphorus Compounds / chemical synthesis
Phosphorus Radioisotopes
Receptors, G-Protein-Coupled / agonists*
Receptors, Lysosphingolipid / agonists*
Structure-Activity Relationship

Substances

Ligands
Organophosphonates
Organophosphorus Compounds
Phosphorus Radioisotopes
Receptors, G-Protein-Coupled
Receptors, Lysosphingolipid