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A novel thiazole drug molecule for hospital disinfection and its preparation method

A technology of drug molecules and thiazoles, which is applied in botany equipment and methods, chemicals for biological control, disinfectants, etc., can solve the problems that affect the appearance of medical devices, low molecular polarity, low solubility, etc., and achieve Good force, good inhibition, safe reaction and operation effect

Active Publication Date: 2020-04-10
THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the quaternary ammonium salt disinfectant has a significant disadvantage, that is, as a salt compound, the content of quaternary ammonium salt in the disinfectant is relatively high. If it is not cleaned on the surface of medical equipment, it will leave salt stains and affect medical treatment. The beauty of the device; we found a pyrimidothiazole compound with good antibacterial activity, which can produce a good antibacterial effect in a small dose. As a non-salt compound, it will not remain on the medical device
[0006] In view of the shortcomings of quaternary ammonium salts, our research team invented a non-salt disinfectant drug. At the beginning, we invented a pyrimidothiazole compound with this structure: After testing, it is found that the compound has good antibacterial effect; but after further research, it is found that the compound has two aromatic rings, so the molecular polarity is small, and the solubility in ethanol is small, so we plan to synthesize the compound The method and compound structure are further optimized, making it soluble in ethanol, which is convenient for use in hospital disinfection centers

Method used

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  • A novel thiazole drug molecule for hospital disinfection and its preparation method
  • A novel thiazole drug molecule for hospital disinfection and its preparation method
  • A novel thiazole drug molecule for hospital disinfection and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0029]

[0030]In a reaction device with a water separator, add 13.5g of 4-methylacetophenone, 11.5g of thiourea and 38g of elemental iodine into 200mL of N,N-dimethylformamide, slowly raise the temperature to 100°C, and react for 2h Finally, 120 mL of the reaction solvent was aliquoted under vacuum conditions, the reaction system was in a viscous state, cooled to room temperature, 150 mL of ether was added to the reaction system, a large amount of solids were precipitated, the reaction solution was filtered, all the filter cake was added to 300 mL of water, and heated to reflux , reacted for 30 minutes, cooled to 10 ° C, a large amount of solids precipitated, filtered the reaction again, and dried the filter cake to obtain 17 g of compound 4-(4-methylbenzene)-thiazol-2-amine; 1 H NMR (400MHz, DMSO-d 6 ):δ7.67(dd,J 1 =8.0Hz,J 2 =4.0Hz, 2H), 7.16(d, J=8.0Hz, 2H), 7.01(s, 2H), 6.90(s, 1H), 2.35(s, 3H); 13 C NMR (400MHz, DMSO-d 6 ): 168.2, 149.9, 136.4, 132.3, 129.0, 125.5...

Embodiment 2

[0032] In a reaction device with a water separator, add 13.5g of 4-methylacetophenone, 11.5g of thiourea and 25g of elemental iodine into 170mL of N,N-dimethylformamide, slowly raise the temperature to 100°C, and react for 2h Finally, 120 mL of the reaction solvent was aliquoted under vacuum conditions, the reaction system was in a viscous state, cooled to room temperature, 150 mL of ether was added to the reaction system, a large amount of solids were precipitated, the reaction solution was filtered, all the filter cake was added to 300 mL of water, and heated to reflux , reacted for 30 minutes, cooled to 10 ° C, a large amount of solids precipitated, filtered the reaction again, and dried the filter cake to obtain 14.3 g of compound 4-(4-methylbenzene)-thiazol-2-amine; 1 H NMR (400MHz, DMSO-d 6 ):δ7.67(dd,J 1 =8.0Hz,J 2 =4.0Hz, 2H), 7.16(d, J=8.0Hz, 2H), 7.01(s, 2H), 6.90(s, 1H), 2.35(s, 3H); 13 C NMR (400MHz, DMSO-d 6 ): 168.2, 149.9, 136.4, 132.3, 129.0, 125.5, 100.6, ...

Embodiment 3

[0034] In a reaction device with a water separator, add 13.5g of 4-methylacetophenone, 7.6 thiourea and 38g of elemental iodine into 200mL of N,N-dimethylformamide, slowly raise the temperature to 100°C, and react for 2h Finally, 120 mL of the reaction solvent was aliquoted under vacuum conditions, the reaction system was in a viscous state, cooled to room temperature, 150 mL of ether was added to the reaction system, a large amount of solids were precipitated, the reaction solution was filtered, all the filter cake was added to 300 mL of water, and heated to reflux , reacted for 30 minutes, cooled to 10°C, a large amount of solids were precipitated, the reaction was filtered again, and the filter cake was dried and separated by silica gel column chromatography to obtain 9.2 g of compound 4-(4-methylbenzene)-thiazol-2-amine; 1 H NMR (400MHz, DMSO-d 6 ):δ7.67(dd,J 1 =8.0Hz,J 2 =4.0Hz, 2H), 7.16(d, J=8.0Hz, 2H), 7.01(s, 2H), 6.90(s, 1H), 2.35(s, 3H); 13 C NMR (400MHz, DMSO-d ...

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Abstract

The invention discloses a thiazole drug molecule for hospital disinfection and a preparation method thereof, and belongs to the technical field of antibacterial drug synthesis. The key point of the technical scheme of the invention is that the thiazole drug molecule has a structure as shown in the specification; by optimizing the structure of the original thiazole drug molecule, and replacing an aromatic ring in the original structure with a fatty ether alkane, the polarity of the compound is increased and the component is better soluble in ethanol; the reaction between 4-methyl acetophenone and thiourea instead of 4-methyl acetophenone and a toxic amino cyanogen compound is used for obtaining a key intermediate 4-(4-methyl benzene)-thiazole-2-amine, so that the reaction operation is safer; the compound obtained in the invention has a better inhibitory effect on staphylococcus aureus; and by calculation, that the novel thiazole compound has a better effect on staphylococcus aureus targets than the original thiazole compound is found.

Description

technical field [0001] The invention belongs to the technical field of disinfection and bactericidal drug synthesis, and in particular relates to a novel thiazole drug molecule used for hospital disinfection and a preparation method thereof. Background technique [0002] The disinfection supply center is an important department in the hospital. It is the department responsible for the cleaning, disinfection, sterilization and supply of sterile items for all reusable medical instruments, utensils and articles in the hospital. By strengthening the cleaning management of reusable instruments, the safety of hospital diagnosis and treatment activities can be guaranteed. It can be seen that the disinfection supply center is the "heart" of the hospital. For all kinds of reusable devices, appropriate cleaning technology must be selected to ensure the quality of medical devices. [0003] In order to reduce the chance of nosocomial infection, it is necessary to do a good job of disin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D513/04A01N43/90A01P1/00
CPCA01N43/90C07D513/04
Inventor 刘芳芳王英姿冯海瑕乔艳
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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