title: Evaluation of polyhydroxybenzophenones as α-glucosidase inhibitors.
abstract: This experiment was designed to synthesize 18 kinds of polyhydroxybenzophenones by using Friedel-Crafts reaction, and to measure the inhibitory activity on α-glucosidase with p-nitrophenyl-β-D-galactopyranoside (PNPG) as a substrate. Here, acarbose (IC(50)  = 1674.75 µmol L(-1) ) was used as the reference inhibitor. The results demonstrated that most of the target compounds had remarkable inhibitory activities on α-glucosidase. Among all these compounds, 2,4,4',6-butahydroxydiphenylketone (11) was found to be the most potent α-glucosidase inhibitor with an IC(50) value of 10.62 µmol L(-1) . In addition, we found these compounds were competitive inhibitors through the kinetic analysis. The results suggested that such compounds might be utilized for the development of new candidates for diabetes treatment.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, PR China.
authors.forename: Xuesen
authors.initials: X
authors.lastname: Hu
authors.forename: Yang
authors.initials: Y
authors.lastname: Xiao
authors.forename: Jianlong
authors.initials: J
authors.lastname: Wu
authors.forename: Lin
authors.initials: L
authors.lastname: Ma
mesh_terms: D001577:Benzophenones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D007700:Kinetics; D015394:Molecular Structure; D009598:Nitrophenylgalactosides / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001577:Benzophenones; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D009598:Nitrophenylgalactosides; C059200:4-nitrophenylgalactoside