Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase.

Paul Hebeisen,Wolfgang Haap,Bernd Kuhn,Peter Mohr,Hans Peter Wessel,Ulrich Zutter,Stephan Kirchner,Armin Ruf,Jörg Benz,Catherine Joseph,Rubén Alvarez-Sánchez,Marcel Gubler,Brigitte Schott,Agnes Benardeau,Effie Tozzo,Eric Kitas

Bioorganic & Medicinal Chemistry Letters（2011）

引用 15|浏览22

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摘要

Compound 19 is representative of a novel sulfonylureido pyridine series that yielded potent inhibitors of fructose-1,6-bisphosphatase, showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes.

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关键词

Fructose-1,6-bisphosphatase,FBPase,Allosteric inhibition,Structure–activity studies,X-ray crystallography,Genotoxicity,Glucose reduction,db/db Mouse model

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