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

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 IC50 of 0.57 μM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

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