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Application of Click Chemistry and De-Click Chemistry in Quantitative Drug Synthesis and Release

A technology of click chemistry and medicine, applied in chemical instruments and methods, organic chemistry, compounds containing elements of group 3/13 of the periodic table, etc., to achieve fast reaction speed, high reaction yield, and mild reaction conditions

Active Publication Date: 2020-08-28
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, although Click chemistry has been widely used, the simultaneous use of Click chemistry and Declick chemistry to achieve rapid quantitative assembly and quantitative release of drugs has not been reported.

Method used

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  • Application of Click Chemistry and De-Click Chemistry in Quantitative Drug Synthesis and Release
  • Application of Click Chemistry and De-Click Chemistry in Quantitative Drug Synthesis and Release
  • Application of Click Chemistry and De-Click Chemistry in Quantitative Drug Synthesis and Release

Examples

Experimental program
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Effect test

Embodiment 1

[0071] To 2 mL of PB buffer (10 mM, pH=7.4, 1 mM CTAB), add 10 μL of NBD-Cl stock solution with a concentration of 2 mM, and then add 1 μL of GSH with a concentration of 20 mM, and test the change of its absorption spectrum with time, as shown in figure 2 As shown, the absorption at 343nm decreased gradually, the absorption at 421nm increased gradually, and the reaction equilibrium was reached in about 3 minutes. After the reaction reaches equilibrium, add 10 μL of Cys or Hcy with a concentration of 20 mM, such as Figure 6 , as shown in 7, the absorption at 421nm decreases gradually, and the absorption peak at 470nm gradually increases, and reaches equilibrium in about 3 minutes, as Figure 15 ,16, the absorption spectrum when it reaches equilibrium is basically the same as the absorption spectrum when NBD-Cl (10 μM) is added to Cys or Hcy (10 μM).

[0072] To 2 mL of PB buffer (10 mM, pH=7.4, 1 mM CTAB) system, add 10 μL of NBD-Cl stock solution with a concentration of 2 m...

Embodiment 2

[0074] To 2mL of PB buffer (10mM, pH=7.4, 2.5mM CTAB) system, add 10μL of NBD-Cl stock solution with a concentration of 2mM, and then add 1μL of GSH with a concentration of 20mM, and test the change of its absorption spectrum with time, 343nm The absorption at 421nm decreased gradually, and the absorption at 421nm increased gradually, and the reaction equilibrium was reached in about 3 minutes. After the reaction reaches equilibrium, add 10 μL of Cys or Hcy with a concentration of 20mM, the absorption at 421nm gradually decreases, the absorption peak at 470nm gradually increases, and reaches equilibrium in about 3 minutes. The absorption spectrum when it reaches equilibrium is the same as that of NBD-Cl( 10μM) when Cys or Hcy (10μM) was added, the absorption spectra were basically the same.

[0075] To 2mL of PB buffer (10mM, pH=7.4, 1mM CTAB) system, add 10μL of NBD-Cl stock solution with a concentration of 2mM, then add 1μL of GSH with a concentration of 20mM, and test the c...

Embodiment 3

[0077] To 2mL of PB buffer (10mM, pH=7.4, 5mM CTAB) system, add 10μL of NBD-Cl stock solution with a concentration of 2mM, then add 1μL of GSH with a concentration of 20mM, and test the change of its absorption spectrum with time, at 343nm The absorption at 421nm gradually decreased, and the absorption at 421nm gradually increased, and the reaction equilibrium was reached in about 3 minutes. After the reaction reaches equilibrium, add 10 μL of Cys or Hcy with a concentration of 20mM, the absorption at 421nm gradually decreases, the absorption peak at 470nm gradually increases, and reaches equilibrium in about 3 minutes. The absorption spectrum when it reaches equilibrium is the same as that of NBD-Cl( 10μM) when Cys or Hcy (10μM) was added, the absorption spectra were basically the same.

[0078]To 2mL of PB buffer (10mM, pH=7.4, 1mM CTAB) system, add 10μL of NBD-Cl stock solution with a concentration of 2mM, then add 1μL of GSH with a concentration of 20mM, and test the chang...

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Abstract

The invention provides an application of click chemistry and declick chemistry to quantitative synthesis and release of a drug. On the basis of a template molecule, the quantitative assembling and release of sulfydryl-containing drug molecules such as N-acetyl-L-cysteine (NAC), glutathione (GSH), methimazole, tiopronin, captopril and mercaptopurine can be realized by utilizing the click chemistryand declick chemistry, and the assembling and release process of the sulfydryl-containing drug molecules can be monitored by utilizing the fluorescence variation in the process. The template moleculecan rapidly react with the sulfydryl-containing drug molecules in a ratio of 1:1 in the presence of the surfactant, the template molecule and the molecule after the assembling of the sulfydryl-containing drug molecules can rapidly have declick-chemistry in the presence of a nucleophilic reagent to release the sulfydryl-containing drug molecules. The fluorescence is varied in the sulfydryl-containing drug molecule release process, so that the release of the drug molecules can be conveniently monitored by utilizing the fluorescence variation of the sulfydryl-containing drug molecule.

Description

technical field [0001] The invention relates to the application field of click chemistry and de-click chemistry, in particular to an application of click chemistry and de-click chemistry in the quantitative synthesis and release of drugs. Background technique [0002] Click chemistry, also translated as "link chemistry", "dynamic combinatorial chemistry" and "speed-dating combinatorial chemistry", is an organic synthesis concept first introduced by American chemist K B Sharpless in 2001. The reaction The process is as simple, efficient, practical, and controllable as clicking a mouse. The main purpose is to form carbon-heteroatom bonds with high selectivity through the splicing of different units under mild conditions, and quickly and accurately synthesize various target molecules. In the context of green synthesis and the era of atomic economy, the concept of Click chemistry has made great contributions in the field of chemical synthesis, and it has been widely used in many...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D271/12C07F5/02
CPCC07D271/12C07F5/022
Inventor 孙远强梁增强屈凌波陈晓岚
Owner ZHENGZHOU UNIV