Optimization of a Potent, Orally Active S1P(1) Agonist Containing a Quinolinone Core

[Image: see text] The optimization of a series of S1P(1) agonists with limited activity against S1P(3) is reported. A polar headgroup was used to improve the physicochemical and pharmacokinetic parameters of lead quinolinone 6. When dosed orally at 1 and 3 mg/kg, the azahydroxymethyl analogue 22 ach...

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Detalhes bibliográficos
Main Authors: Harrington, Paul E., Croghan, Michael D., Fotsch, Christopher, Frohn, Mike, Lanman, Brian A., Pennington, Lewis D., Pickrell, Alexander J., Reed, Anthony B., Sham, Kelvin K. C., Tasker, Andrew, Arnett, Heather A., Fiorino, Michael, Lee, Matthew R., McElvain, Michele, Morrison, Henry G., Xu, Han, Xu, Yang, Zhang, Xuxia, Wong, Min, Cee, Victor J.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025730/
https://ncbi.nlm.nih.gov/pubmed/24900374
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200252b
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