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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Bibliografski detalji
Glavni autori: 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.
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2011
Online pristup: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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