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Method for promoting carbon monoxide release of carbon monoxide-releasing molecules and preventing sedimentation

A technology of carbon monoxide and release agent, which is applied in the field of medicinal chemistry, can solve the problems of slow release rate of carbon monoxide, and achieve the effects of easy control of timing and rate, promotion of release, and promotion of production

Inactive Publication Date: 2015-08-05
JIAXING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the release rate of carbon monoxide induced by amino acids and their derivatives or drug molecules is relatively slow, and a certain amount of precipitation will also be produced during the reaction.

Method used

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  • Method for promoting carbon monoxide release of carbon monoxide-releasing molecules and preventing sedimentation
  • Method for promoting carbon monoxide release of carbon monoxide-releasing molecules and preventing sedimentation
  • Method for promoting carbon monoxide release of carbon monoxide-releasing molecules and preventing sedimentation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Compound 1 (17mg, 34mmol) was added to 2.4mL DMSO, dissolved and added to the reaction tube, and an appropriate amount of amino acid or drug molecule aqueous solution (0.1mL, 1.035mol L -1 ,[Compound 1]:[amino acid or drug molecule]=1:3) and 0.5mL aqueous solution, and measure the infrared (Varian Scimitar 600) every once in a while. The experimental process of adding EDTA to this system is similar to the above process, except that 0.1mL EDTA-2Na aqueous solution (3.45mol L -1 ), and the added aqueous solution is 0.4mL, ensuring that the final solution is 3.0mL.

[0030] After adding proline or tiopronin to compound 1, the infrared spectrum changes obviously, such as figure 1 and 3 As shown, compound 1 is in 2068, 2031, 1989cm -1 There are three obvious carbonyl absorption peaks, and these infrared characteristic peaks are obviously weakened after adding proline or tiopronin. It can be seen that the carbonyl group of compound 1 is gradually reduced and released as c...

Embodiment 2

[0033] Compound 2 (14mg, 34mmol) was added to 2.4mL DMSO, dissolved and added to the reaction tube, and an appropriate amount of drug molecule aqueous solution (0.1mL, 1.035mol L -1 ,[Compound 1]:[amino acid or drug molecule]=1:3) and 0.5mL aqueous solution, and measure the infrared (Varian Scimitar 600) every once in a while. The experimental process of adding EDTA to this system is similar to the above process, except that 0.1mL EDTA-2Na aqueous solution (3.45mol L -1 ), and the added aqueous solution is 0.4mL to ensure that the final solution is 3.0mL.

[0034] After compound 2 was added tiopronin, the infrared spectrum changed significantly, such as Figure 5 As shown, compound 2 is at 2068, 2031, 1989cm -1 There are three obvious carbonyl absorption peaks, and these infrared characteristic peaks are obviously weakened after adding tiopronin. This shows that after the addition of tiopronin, the characteristic peak of the carbonyl group of compound 2 gradually weakens an...

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Abstract

The invention discloses a method for promoting carbon monoxide release of carbon monoxide-releasing molecules (CORM) and preventing sedimentation and belongs to the technical field of medical chemistry. The method particularly comprises the following steps: dissolving CO releasing molecules in dimethyl sulfoxide, and adding amino acid, or derivatives thereof, or medicine molecules and an EDTA water solution. After adding of EDTA, generation of CO is effectively promoted, and sedimentation in reaction can be quickly removed. The method has good university; compounds related to the reaction have excellent biocompatibility; and after release of CO, sedimentation can be quickly and effectively prevented, and the CO release time and rate can be easily controlled.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a method for promoting a carbon monoxide releasing agent to release carbon monoxide and preventing precipitation from forming. technical background [0002] Carbon monoxide (CO) is a biologically active small molecule in the human body. Like its analog NO, CO plays very important physiological and pathological roles in organisms, such as dilating blood vessels, inhibiting reperfusion injury, anti-apoptosis, anti-proliferation, anti-oxidation, antibacterial, etc. To explore the medicinal potential of this diatomic molecule, its precise on-site release will be a very critical issue. Transition metal carbonyls are a large class of organometallic compounds that can lead to the departure of a carbonyl group (CO) under appropriate conditions, such as light irradiation, substitution reactions, redox induction, etc. Utilizing these properties of metal carbonyl compounds, so...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/295A61K47/18A61P9/00A61P37/06A61P29/00
Inventor 刘小明姜秀娟陈丽梅张佳瑶龙莉
Owner JIAXING UNIV
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