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

      Bioorganic & Medicinal Chemistry Letters
      Allosteric Regulation, Animals, Enzyme Inhibitors, chemistry, pharmacokinetics, pharmacology, Fructose-Bisphosphatase, antagonists & inhibitors, Models, Molecular, Rats, Sulfonamides

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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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