837-60-5Relevant academic research and scientific papers
Evaluation of polyhydroxybenzophenones as α-glucosidase inhibitors
Hu, Xuesen,Xiao, Yang,Wu, Jianlong,Ma, Lin
, p. 71 - 77 (2011)
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 (IC50a= a1674.75aaμmolaL-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 IC50 value of 10.62aaμmolaL-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. A series of polyhydroxybenzophenones was synthesized and evaluated as α-glucosidase inhibitors. Compound 11 was found to be the most potent inhibitor. Copyright
Synthetic method of benzophenone type compound catalyzed by boron trifluoride
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Paragraph 0030; 0034, (2018/10/19)
The invention provides a synthetic method of benzophenone type compound catalyzed by boron trifluoride. The method comprises the following specific steps: adding substituted benzoic acid, a resorcinolderivative and a catalyst boron trifluoride diethyl etherate to a reaction vessel, gradually raising the temperature to 95-120 DEG C, performing reaction for 10-30 min, then performing dissolution with ethyl acetate, performing washing with an equal amount of saturated sodium bicarbonate, and performing drying, recrystallization and decolorization to obtain the benzophenone type compound. The technical scheme provided by the invention has the advantages that the operation is simple and convenient; the substituted benzoic acid and the resorcinol derivative are taken as raw materials to synthesize the benzophenone type compound in one step, thereby reducing the production cost; reaction conditions are mild; the by-product is water which is friendly to the environment; the atom utilization ratio is high; the reaction post-treatment is simple; and the yield can reach 90% or above.
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors
Wu, Jianlong,Hu, Xuesen,Ma, Lin
experimental part, p. 449 - 452 (2012/01/04)
A series of polyhydroxy benzophenone were synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of the target compounds had remarkable inhibitory activities on mushroom tyrosinase. Among all these compounds, 2,3,4,3′,4′,5′-hexahydroxy-diphenylketone 10 was found to be the most potent tyrosinase inhibitor with IC50 value of 1.4 μM. In addition, the inhibition kinetics analyzed by Lineweaver-Burk plots revealed that such compounds were competitive inhibitors. These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders.
