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Abstract

A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53, with an IC(50) of 0.57microM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

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PubMed ID:: 16446092

DOI:: 10.1016/j.bmcl.2006.01.014

ScienceOpen disciplines: Chemistry

Keywords: Allosteric Regulation,Animals,Enzyme Inhibitors,chemistry,pharmacokinetics,pharmacology,Fructose-Bisphosphatase,antagonists & inhibitors,Models, Molecular,Rats,Sulfonamides

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ScienceOpen disciplines: Chemistry

Keywords: Allosteric Regulation, Animals, Enzyme Inhibitors, chemistry, pharmacokinetics, pharmacology, Fructose-Bisphosphatase, antagonists & inhibitors, Models, Molecular, Rats, Sulfonamides

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.

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