Concepedia

Oxazole phosphonic acids as fructose 1,6-bisphosphatase inhibitors with potent glucose-lowering activity

Qun Dang, Srinivas Rao Kasibthatla, Tao Jiang, Frank Taplin, Tony Gibson, Scott Potter, Paul D. van Poelje, Mark D. Erion

MedChemComm · 2011 · 19 citations · 19 references

DOI

Concepts

Abstract

Phosphonic acid-containing oxazoles were discovered as potent inhibitors of fructose 1,6-bisphosphatase. Several oxazoles demonstrated significant glucose-lowering activity in rats after intravenous dosing.

References

19

MB06322 (CS-917): A potent and selective inhibitor of fructose 1,6-bisphosphatase for controlling gluconeogenesis in type 2 diabetes

Mark D. Erion, Paul D. van Poelje, Qun Dang et al. · Proceedings of the National Academy of Sciences · 2005 · 162 citations

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Discovery of a Series of Phosphonic Acid-Containing Thiazoles and Orally Bioavailable Diamide Prodrugs That Lower Glucose in Diabetic Animals Through Inhibition of Fructose-1,6-Bisphosphatase

Qun Dang, Yan Liu, Daniel K. Cashion et al. · Journal of Medicinal Chemistry · 2010 · 160 citations · Full text

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Discovery of Potent and Specific Fructose-1,6-Bisphosphatase Inhibitors and a Series of Orally-Bioavailable Phosphoramidase-Sensitive Prodrugs for the Treatment of Type 2 Diabetes

Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy et al. · Journal of the American Chemical Society · 2007 · 97 citations

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Structure-Guided Design of AMP Mimics That Inhibit Fructose-1,6-bisphosphatase with High Affinity and Specificity

Mark D. Erion, Qun Dang, M. Rami Reddy et al. · Journal of the American Chemical Society · 2007 · 91 citations

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Inhibition of Fructose 1,6-Bisphosphatase Reduces Excessive Endogenous Glucose Production and Attenuates Hyperglycemia in Zucker Diabetic Fatty Rats

Paul D. van Poelje, Scott Potter, Visvanathan Chandramouli et al. · Diabetes · 2006 · 87 citations

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