Studies on new acidic azoles as glucose-lowering agents in obese, diabetic db/db mice

…, TJ Caggiano, KE Steiner, JJ Fitzgerald Jr…

文献索引：Kees, Kenneth L.; Caggiano, Thomas J.; Steiner, Kurt E.; Fitzgerald, John J.; Kates, Michael J.; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 4 p. 617 - 628

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被引用次数: 51

摘要

Bioisosteric substitution was used as a tool to generate several new structural alternatives to the thiazolidine-2, 4-dione and tetrazole heterocycles as potential antidiabetic agents. Among the initial leads that emerged from this strategy, a family of acidic azoles, isoxazol-3- and-5-ones and a pyrazol-3-one, showed significant plasma glucose-lowering activity (17- 42% reduction) in genetically obese, diabetic db/db mice at a dose of 100 mg/kg/day x4. ...