Use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilm

A technology of aminoimidazole and its derivatives, which is applied in antibacterial drugs, organic active ingredients, pharmaceutical formulations, etc. It can solve the problems of not knowing the significant impact of biofilm activity, reducing the biomass of biofilm and the number of viable bacteria, etc., to achieve good results Pharmacokinetic properties, reduction of treatment difficulty, effects of reducing drug resistance and pathogenicity

Active Publication Date: 2021-06-04
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] CN 201410073627.X provides the use of oxazolidinone compounds in the preparation of medicines, disinfectants or daily chemicals for preventing or inhibiting bacterial biofilm formation or removing bacterial biofilm; the provided oxazolidinone compounds can Effectively preventing or inhibiting the formation of bacterial biofilm, or removing bacterial biofilm, can effectively reduce the biomass and the number of viable bacteria in the biofilm. Can oxazolidinones significantly affect the biofilm activity of Gram-negative bacilli

Method used

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  • Use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilm
  • Use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilm
  • Use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilm

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Embodiment 1

[0085] In order to facilitate the understanding of the above-mentioned technical solution of the present invention, the technical solution of the present invention will be described in detail below through specific usage modes. The preparation of embodiment 1 compound

[0086] Compound (I)

[0087] Add 1.0800g 2-aminoimidazole raw material (5mmol) and 1.07mL benzyl chloroformate raw material (5mmol) successively in a 250mL round bottom flask, then add Et 3 N (5mmol) was used as a base, DCM 5.00mL was used as a solvent, stirred at room temperature, reacted for 8h, and detected by thin layer chromatography (petroleum ether: ethyl acetate = 1:1), after confirming that the reaction was completed, ethyl acetate and Water extraction, repeated three times, take the organic phase and add desiccant anhydrous Na 2 SO 4 , stand still, filter, and evaporate to dryness with a rotary evaporator to obtain a white powder, which is then recrystallized with ethyl acetate and water, filtere...

Embodiment 2

[0141] 1) Early preparation

[0142] a) Preparation of LB culture medium

[0143] Weigh 5.0000g of yeast extract, 10.0000g of tryptone, and 10g of sodium chloride with an analytical balance, put them into a transparent glass bottle, then add 1L of distilled water, mix well, adjust the pH to 7.0 with NaOH, and place in an autoclave Sterilize at 121°C for 20 minutes.

[0144] b) Preparation of compound mother liquor

[0145] Take 0.01 mmol of each compound, dissolve it in an EP tube containing 1 mL of ethanol solution, and then dilute it five times, take 100 μL of the compound solution in an EP tube containing 400 μL of ethanol solution, and obtain a compound with a concentration of 0.2 mmol / L solution.

[0146] c) Preparation of bacterial solution

[0147] Use a sterile inoculation loop to inoculate the bacteria in the cryopreservation tube into a centrifuge tube filled with 3-5mL LB culture solution, place the strain in a shaking incubator, and incubate at 37°C, 120r / min f...

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Abstract

The invention relates to the technical field of new uses of compounds, and mainly provides the use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilms. The present invention provides 2-aminoimidazole derivatives or pharmaceutically acceptable salts thereof or compositions thereof in the purposes in the preparation of the medicine of inhibiting bacterial biofilm activity, degrading bacterial biofilm, destroying bacterial biofilm, described 2-aminoimidazole The derivative has a structure shown in the following formula (I): formula (I), wherein, R is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, haloalkyl, haloalkenyl, alkylamino, alkane Oxygen, arylalkoxy, aryl-O-alkyl, aryl-NH-alkyl, arylalkenyl, arylalkyl or arylalkynyl; R 1 , R 2 , R 3 and R 4 Each is independently hydrogen, alkyl, alkenyl, alkynyl, halogen, haloalkyl, alkoxy, aryl, or arylalkyl.

Description

technical field [0001] The invention belongs to the technical field of new uses of compounds, and in particular relates to the use of 2-aminoimidazole derivatives in the preparation of active drugs for inhibiting bacterial biofilms. Background technique [0002] Bacterial biofilms (Bacterial biofilms, BF) refer to the formation of microbial cells and their secreted polymers that adhere to each other in a matrix composed of nucleic acids, proteins, and polysaccharides. Bacteria group, which can be composed of one or more kinds of bacteria. Its growth mode is corresponding to the planktonic state, and has different biological characteristics compared with planktonic bacteria. Moreover, studies have found that a large number of platelets, cell debris, and various metabolites are attached to the surface of BF. The formation of BF can be roughly divided into four distinct stages, which is a dynamic process, including bacterial colonization stage, aggregation stage, biofilm matu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4168A61P31/04
CPCA61K31/4168
Inventor 杨元勇汤磊杨果程铖
Owner GUIZHOU MEDICAL UNIV
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