Acyl Glucuronide Metabolites of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK)

Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have culminated in the identification of PF-06409577 (1), PF-06885249 (2), and PF-06679142 (3) as potential clinical candidates. Compounds 1–3 are prim...

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Veröffentlicht in:	Journal of medicinal chemistry 2018-08, Vol.61 (16), p.7273-7288
Hauptverfasser:	Ryder, Tim F., Calabrese, Matthew F., Walker, Gregory S., Cameron, Kimberly O., Reyes, Allan R., Borzilleri, Kris A., Delmore, Jake, Miller, Russell, Kurumbail, Ravi G., Ward, Jessica, Kung, Daniel W., Brown, Janice A., Edmonds, David J., Eng, Heather, Wolford, Angela C., Kalgutkar, Amit S.
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Acyls Conjugate acid-base pairs INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY Metabolism Peptides and proteins Rodent models
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