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Method for screening dihydrochalcone compound

A dihydrochalcone and screening method technology, applied in biological testing, material inspection products, etc., can solve problems such as energy-consuming, time-consuming and cost-consuming, and achieve the effect of reducing time and cost

Inactive Publication Date: 2011-07-06
SHANGHAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the traditional method, if m reactants A (A1, A2...Am) containing different derivative groups are combined with n reactants B (B1, B2...Am) with different derivative groups .Bn) are synthesized separately, and chemical synthesis requires m×n times of reactions, purification, activity test, identification and other cumbersome processes
In order to select highly active compounds and repeat the above steps, time-consuming, cost-intensive and energy-intensive

Method used

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  • Method for screening dihydrochalcone compound
  • Method for screening dihydrochalcone compound
  • Method for screening dihydrochalcone compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] a. Prepare 10 kinds of acetophenone compound series A and 10 kinds of benzaldehyde compound series B. The names and corresponding serial numbers of the compounds are shown in Table 1 respectively.

[0026] Table 1 A, B series compound names and corresponding serial numbers

[0027]

[0028]

[0029] Before aldol condensation, A 1 to A 7 , B 1 to B 5 The active phenolic hydroxyl group on the benzene ring is protected by a benzyl group, and the steps are as follows: add 0.05mol hydroxyl-containing acetophenone compound or benzaldehyde compound to a 250mL three-necked flask, dissolve it in 50mL absolute ethanol, and then add 0.035mol K 2 CO 3 , under mechanical stirring, slowly add 0.06mol benzyl chloride dropwise, the molar ratio of hydroxyl-containing acetophenone compounds or benzaldehyde compounds to benzyl chloride is 1:1.2, after the addition is completed, heat to reflux for reaction, TLC tracking reaction to Raw material points disappear. Recover ethanol...

Embodiment 2

[0043] a. Prepare 7 kinds of acetophenone compound series A and 12 kinds of benzaldehyde compound series B. See Table 4 for the compound names and corresponding serial numbers.

[0044] Table 4 A, B series compound names and corresponding serial numbers

[0045]

[0046] Before aldol condensation, A 6 and B 11 The active phenolic hydroxyl group on the benzene ring is protected by a benzyl group, and the steps are as follows: add 0.05molA 6 or B 11 , after dissolving with 50mL absolute ethanol, add 0.035mol K 2 CO 3 , under mechanical stirring, slowly drop 0.06mol benzyl chloride, the hydroxyl-containing A 6 or B 11 The molar ratio of benzyl chloride to benzyl chloride is 1:1.2. After the dropwise addition is completed, the reaction is heated to reflux, and the reaction is tracked by TLC until the raw material point disappears. Recover ethanol by rotary evaporation, add water, and extract with ethyl acetate. The extract was washed twice with 5% NaOH, and then washed ...

Embodiment 3

[0061] Take normal Kunming mice, half male and half female, fasted without water for 14 hours, intraperitoneally injected with 2% alloxan (200 mg / kg) normal saline solution, and resume normal diet after injection. After 72 hours, the blood glucose of mice fasted for 8 hours without food and water was measured, and those whose blood glucose value was greater than 11.1mmol / L were experimentally qualified animal models of diabetes.

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Abstract

The invention relates to a method for screening a dihydrochalcone compound, which comprises the following steps: firstly combining B series of compounds of a plurality of benzaldehyde compounds into a mixture and leading the mixture to react with m types of A series of acetophenone compounds of a ketoaldehyde condensation reactant in sequence to generate corresponding m groups of dihydrochalcone mixtures; combining the m types of A series of compounds into a mixture and leading the mixture to react with B series of single compounds in sequence to generate a plurality of groups of dihydrochalcone mixtures. Respective strongest mixtures are selected from the A series of mixtures and the B series of mixtures to determine the strongest A series of acetophenone compound and the strongest B series of benzaldehyde compound; the strongest A series of acetophenone compound is reacted with a plurality of B series of compounds in sequence, and the strongest B series of benzaldehyde mixture is reacted with the m types of A series of the acetophenone compounds to commonly generate M plus N minus 1 types of dihydrochalcone; and a strongest dihydrochalcone compound secreted and acted by pancreotropichormone is screened, namely a target compound screened by the method.

Description

technical field [0001] The invention relates to a screening method for dihydrochalcone compounds. technical background [0002] As one of the sources of discovering new drugs, natural resources have played an important role in the history of drug development. Active compounds derived from natural products are the material basis for therapeutic effects. Extracting lead compounds from natural sources for synthesis, structural modification and optimization is the key to the research and development of innovative drugs. [0003] Diabetes mellitus is a syndrome of glucose, protein and lipid metabolism disorder caused by lack of insulin in the body or increase of hormones that antagonize insulin, or that insulin cannot exert normal physiological functions in target cells. Traditional oral hypoglycemic drugs have limited curative effect, and basic research on new natural sources of diabetes drugs is an urgent and urgent task. With the in-depth study of the basic theory of diabete...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N33/74
Inventor 雍克岚吕敬慈汤燕金马颖清顾慧娟
Owner SHANGHAI UNIV
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