Sulfonylureido thiazoles as fructose-1, 6-bisphosphatase inhibitors for the treatment of Type-2 diabetes

…, A Paehler, A Benardeau, M Gubler, B Schott…

文献索引：Kitas, Eric; Mohr, Peter; Kuhn, Bernd; Hebeisen, Paul; Wessel, Hans Peter; Haap, Wolfgang; Ruf, Armin; Benz, Joerg; Joseph, Catherine; Huber, Walter; Sanchez, Ruben Alvarez; Paehler, Axel; Benardeau, Agnes; Gubler, Marcel; Schott, Brigitte; Tozzo, Effie Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 2 p. 594 - 599

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被引用次数: 16

摘要

Sulfonylureido thiazoles were identified from a HTS campaign and optimized through a combination of structure–activity studies, X-ray crystallography and molecular modeling to yield potent inhibitors of fructose-1, 6-bisphosphatase. Compound 12 showed favorable ADME properties, for example, F= 70%, and a robust 32% glucose reduction in the acute db/db mouse model for Type-2 diabetes.