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Indole full dione thiosemicarbazone type compound and use thereof in resisting medicament-resistant bacteria

A technology of indoline diketone thiosemicarbazone and compound, applied in antibacterial drugs, organic chemistry, pharmaceutical formulations, etc., can solve medical problems such as bacterial drug resistance, and achieve strong inhibitory effect

Inactive Publication Date: 2014-01-01
NANKAI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the widespread use of antibacterial drugs, the bacterial resistance caused by them has become a medical problem that cannot be ignored.

Method used

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  • Indole full dione thiosemicarbazone type compound and use thereof in resisting medicament-resistant bacteria
  • Indole full dione thiosemicarbazone type compound and use thereof in resisting medicament-resistant bacteria
  • Indole full dione thiosemicarbazone type compound and use thereof in resisting medicament-resistant bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the synthesis of compound Wang-1

[0027]

[0028] Mix 7-chloroindolindione (1.82g, 10mmol) and p-chlorophenylthiosemicarbazide (2.02g, 10mmol) with 5mL acetic acid, reflux in 50mL ethanol-water (5:1) solution for 6h, and then After cooling to room temperature, the ethanol solution was recrystallized to obtain 2.76 g of the target compound with a yield of 76%.

[0029] Likewise, all other compounds Wang-2 to Wang-47 of the present invention can be synthesized.

[0030] The physical and chemical parameters such as yield, melting point and character of target compound are shown in Table 1, and target compound 1 H NMR, 13 The characterization data such as C NMR, infrared spectroscopy, elemental analysis and mass spectrometry are shown in Table 2.

Embodiment 2

[0031] Example 2: Determination of anti-MRSA activity of indolindiketone thiosemicarbazone compounds.

[0032] 1. Experimental materials

[0033] Mueller-Hinton Broth (Beijing Oboxing Biotechnology Co., Ltd.), tryptone (UK OXOID company), yeast extract powder (UK OXOID company), sodium chloride (Sinopharm Chemical Reagent Co., Ltd.), 96-well cell culture plate ( flat bottom) (Corning, U.S.), positive control drug vancomycin (Amresco, U.S.), dimethyl sulfoxide DMSO (Sinopharm Chemical Reagent Co., Ltd.), MHB medium (use an electronic balance to weigh 24 grams of Mueller-Hinton Broth dry powder was dissolved in 1000 ml of distilled water, adjusted to pH 7.2, and sterilized at 121° C. for 20 minutes using an autoclave to prepare). Methicillin-resistant Staphylococcus aureus (MRSA) clinical isolates (chaoyang are clinically isolated drug-resistant strains from Beijing Chaoyang Hospital, 6281, 6-42, 8-21 and 8-24 are clinically isolated drug-resistant strains from the PLA 306 Hosp...

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Abstract

The invention relates to an indole full dione thiosemicarbazone type compound and a use thereof in preparation of anti-medicament-resistant bacteria medicaments. The indole full dione thiosemicarbazone type compound provided by the invention has a very strong effect on inhibiting methicillin-resistant Staphylococcus aurei (MRSA) and vancomycin-resistant enterococci (VRE) and can be used for preparing the novel and effective anti-medicament-resistant bacteria medicaments. The medicaments can be prepared into injections, tablets, pills, capsules, suspensions or emulsions for use. A medicament delivery way can adopt oral medication and transdermal, intravenous or intramuscular injection. The chemical structural formula of the indole full dione derivative provided by the invention is as shown in formula (I), and in the formula, R1 is o-CH3, o-OCH3, o-F, m-CH3, m-OCH3, m-F, m-Cl, p-CH3, p-OCH3, p-F, p-Cl, p-Br or H; and R2 is CH3, F, Cl, Br, I or H.

Description

technical field [0001] The invention relates to indolindione thiosemicarbazone compounds and their application in the preparation of anti-drug-resistant bacteria drugs, especially for methicillin-resistant Staphylococcus aureus (methicillin-resistant Staphylococcus aureus, MRSA) and vancomycin-resistant Super drug-resistant bacteria such as vancomycin-resistant Enterococcus (VRE) have a strong inhibitory effect. Background technique [0002] Antibiotics are the greatest invention of the 20th century, freeing humans from the deadly threat of bacterial infections. However, with the widespread use of antibacterial drugs, the bacterial resistance caused by them has become a medical problem that cannot be ignored. [0003] Since British scientist Jevons MP et al. (Br.Med.J.1961,1,124-125) discovered methicillin-resistant Staphylococcus aureus (methicillin-resistant Staphylococcus aureus, MRSA) for the first time in 1961, MRSA infection has been surprisingly The speed is spreadi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/40A61K31/404A61P31/04
CPCC07D209/40
Inventor 王建国张立新李在顺郭徽王伟民代焕琴李正名宋福行
Owner NANKAI UNIV
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