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 IC 50 of 0.57 μM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorg. Med. Chem. Lett 2006-04, Vol.16 (7), p.1807-1810
Hauptverfasser:	Lai, Chunqiu, Gum, Rebecca J., Daly, Melissa, Fry, Elizabeth H., Hutchins, Charles, Abad-Zapatero, Celerino, von Geldern, Thomas W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Allosteric regulator Animals Benzoxazole benzenesulfonamide Biological and medical sciences Enzyme inhibitor Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Fructose-1,6-bisphosphatase Fructose-Bisphosphatase - antagonists & inhibitors General and cellular metabolism. Vitamins Medical sciences Models, Molecular Pharmacology. Drug treatments Rats Structure–activity studies Sulfonamides - chemistry Sulfonamides - pharmacokinetics Sulfonamides - pharmacology X-ray crystallography
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Beschreibung
Zusammenfassung:	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 0.57 μM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.01.014