High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators

We previously identified phenylquinoxalinone CFTR(act)-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC(50) of ∼200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here, structure v–activity studies were done on 36 synthesize...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Son, Jung-Ho, Zhu, Jie S., Phuan, Puay-Wah, Cil, Onur, Teuthorn, Andrew P., Ku, Colton K., Lee, Sujin, Verkman, Alan S., Kurth, Mark J.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2017
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5463557/
https://ncbi.nlm.nih.gov/pubmed/28230981
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01759
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