title: Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase.
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.
authors.affiliation: Metabolic Disease Research, GPRD, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. Chunqiu.lai@abbott.com
authors.forename: Chunqiu
authors.initials: C
authors.lastname: Lai
authors.forename: Rebecca J
authors.initials: RJ
authors.lastname: Gum
authors.forename: Melissa
authors.initials: M
authors.lastname: Daly
authors.forename: Elizabeth H
authors.initials: EH
authors.lastname: Fry
authors.forename: Charles
authors.initials: C
authors.lastname: Hutchins
authors.forename: Celerino
authors.initials: C
authors.lastname: Abad-Zapatero
authors.forename: Thomas W
authors.initials: TW
authors.lastname: von Geldern
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006597:Fructose-Bisphosphatase / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D051381:Rats; D013449:Sulfonamides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013449:Sulfonamides; D006597:Fructose-Bisphosphatase