Title of article :
Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase
Author/Authors :
Chunqiu Lai، نويسنده , , Rebecca J. Gum، نويسنده , , Melissa Daly، نويسنده , , Elizabeth H. Fry، نويسنده , , Charles Hutchins، نويسنده , , Celerino Abad-Zapatero، نويسنده , , Thomas W. von Geldern، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2006
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 IC50 of 0.57 μM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.
Keywords :
X-ray crystallography , 6-bisphosphatase , Enzyme inhibitor , Allosteric regulator , Benzoxazole benzenesulfonamide , fructose-1 , Structure–activity studies
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
