Article ID Journal Published Year Pages File Type
5158247 European Journal of Medicinal Chemistry 2017 62 Pages PDF
Abstract
A series of novel berberine derivatives, as AMPK indirect activators, was designed, synthesized, and biologically evaluated for their anti-diabetic activity. Optimized compound 4bq stimulated glucose consumption (2.2-fold) in L6 myotubes, reduced hepatocytes gluconeogenesis (by 85%) and improved pharmacokinetic profiles (bioavailability 45%) compared to berberine. In a db/db mice model compound 4bq lowered fasting blood glucose at a dose of 120 mg/kg/day, and compound 4bq exhibited no obvious hERG inhibition (IC50 > 10 μM).159
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Physical Sciences and Engineering Chemistry Organic Chemistry
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