Application of click chemistry and declick chemistry to quantitative synthesis and release of drug

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...

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.

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