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New application of nitro-styrene derivatives in inhibition of fructose-1,6-bisphosphatase

A technology of nitrostyrene and diphosphatase, applied in the direction of active ingredients of nitro compounds, active ingredients of hydroxyl compounds, medical preparations containing active ingredients, etc., can solve the problem of not reducing antidiabetic drugs

Active Publication Date: 2014-11-19
HUAZHONG NORMAL UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

So far, no antidiabetic drugs that reduce endogenous glucose production have been used clinically

Method used

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  • New application of nitro-styrene derivatives in inhibition of fructose-1,6-bisphosphatase
  • New application of nitro-styrene derivatives in inhibition of fructose-1,6-bisphosphatase
  • New application of nitro-styrene derivatives in inhibition of fructose-1,6-bisphosphatase

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specific Embodiment approach

[0018] In order to illustrate that such nitrostyrene compounds do have a good inhibitory effect on the target enzyme fructose-1,6-bisphosphatase that can be used to treat type II diabetes, we carried out enzymatic tests on the above compounds, and the specific implementation methods are as follows:

[0019] Fructose-1,6-bisphosphatase is an important regulatory enzyme of gluconeogenesis in the human body, which can catalyze the hydrolysis of fructose-1,6-bisphosphate into fructose-6-phosphate and inorganic phosphate. Inorganic phosphoric acid can form a blue-green complex with a mixture of basic dye malachite green and ammonium molybdate in the presence of polyhexenol. The reaction system is 50mM Tric-HCl pH7.4, 0.8mM MgCl 2 , FBPase11.2μg / ml, 0.4mM FBP (fructose-1,6-bisphosphate), appropriate concentration gradient inhibitors (compounds numbered below), enzymatic hydrolysis at 37°C for 5min, and 1M perchloric acid to terminate the enzymatic reaction , using the endpoint meth...

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Abstract

The invention provides a new application of nitro-styrene derivatives having a structure shown in a general formula I, and a good effect of inhibiting fructose-1,6-bisphosphatase, with the lowest IC up to 0.36muM. When R1, R2, R3, R4 and R5 are hydrogen, R3 represents hydrogen, methoxyl, hydroxyl, borono, fluorine, chlorine, bromine, amino, phenyl, methyl, ethyl, isopropyl, tert-butyl, trifluoromethyl, amino, cyano, methylthio, benyloxyl, carboxyl or 2-nitroethenyl; when R1 and R2 are hydrogen, R3 is methoxyl, and R5 is nitro, R4 represents hydroxyl or methoxymethanoyl; when R1, R2 and R5 are hydrogen, R3 represents methyoxyl, and R4 represents methyoxyl or hydroxyl; when R1 and R4 are hydrogen and R5 is nitro, R2 and R3 represent hydroxyl; and when R2 is 2-nitroethenyl, R1, R3, R4 and R5 are hydrogen or hydroxyl.

Description

technical field [0001] The invention relates to a new application of a class of nitrostyrene inhibitors, which have a better inhibitory effect on the target enzyme fructose-1,6-bisphosphatase used for treating type II diabetes. Background technique [0002] Diabetes mellitus is a chronic metabolic disease regulated by multiple genes, mainly manifested as persistent hyperglycemia and glucosuria. Sustained hyperglycemia can lead to many complications, such as retinal, renal, nervous system lesions and vascular complications. According to the statistics of the International Diabetes Federation (IDF), there are currently about 230 million diabetic patients in the world, accounting for almost 6% of the total number of adults in the world. The incidence of diabetes in my country is increasing rapidly. It is predicted that there are more than 92 million diabetic patients in my country, and about 148 million people are high-risk groups of diabetes. [0003] Diabetes is divided int...

Claims

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Application Information

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IPC IPC(8): A61K31/085A61K31/05A61K31/265A61K31/04A61K31/69A61K31/10A61K31/277A61P3/10
Inventor 万坚韩新亚陈海峰朱昊冯玲玲任彦亮池波
Owner HUAZHONG NORMAL UNIV
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