Bioorganic & Medicinal Chemistry Letters 2006-04-01

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

Chunqiu Lai, Rebecca J Gum, Melissa Daly, Elizabeth H Fry, Charles Hutchins, Celerino Abad-Zapatero, Thomas W von Geldern

Index: Bioorg. Med. Chem. Lett. 16 , 1807, (2006)

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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.