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Aryl ketone peptide deformylase inhibitor and application thereof in antibacterial and anti-tumor aspects

A technology of peptide deformylase and inhibitor, which is applied in the field of aryl ketone peptide deformylase inhibitor and its application in antibacterial and antitumor, can solve the problems of metabolic toxicity and no inhibitory activity, and achieve Good anti-tumor activity, good inhibitory activity, novel structure effect

Active Publication Date: 2021-08-06
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the current PDF inhibitors only have good antibacterial activity against Gram-positive bacteria, but basically have no inhibitory activity against Gram-negative bacteria, and there are metabolic toxicity problems in vivo

Method used

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  • Aryl ketone peptide deformylase inhibitor and application thereof in antibacterial and anti-tumor aspects
  • Aryl ketone peptide deformylase inhibitor and application thereof in antibacterial and anti-tumor aspects
  • Aryl ketone peptide deformylase inhibitor and application thereof in antibacterial and anti-tumor aspects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 Aryl ketone peptide deformylase inhibitor and its synthesis method

[0029] The aryl ketone peptide deformylase inhibitor of the present implementation has a structure shown in formula (1) or formula (2):

[0030]

[0031] In the formula, R 1 For cyano, acetonitrile, hydroxyl; R 2 For hydrogen, C1-C6 alkanyl and cycloalkyl or aryl.

[0032]

[0033] In the formula, R 3 For pyridine ring, thiazole ring.

[0034] The aryl ketone peptide deformylase inhibitors of this implementation include a total of 22 compounds, wherein compounds 1, 2, 3, 4, 5, 6, 7, 8, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, and 21 belong to the structure shown in formula (1), and compounds 9 and 10 belong to the structure shown in formula (2). The structural formulas and molecular weights of these compounds are shown in Table 1.

[0035] Structural formula and molecular weight of table 1 aryl ketone peptide deformylase inhibitor

[0036]

[0037]

[0038]

[0039] ...

Embodiment 2

[0218] The antibacterial activity of embodiment 2 aryl ketone peptide deformylase inhibitors (compound 1-22) (minimum antibacterial MIC determination)

[0219] (1) Clinical isolates: Methicillin-resistant Staphylococcus aureus, Klebsiella pneumoniae, P. aeruginosa and Acinetobacter baumannii ); the above strains were all from the First Affiliated Hospital of Sun Yat-sen University in South China. Quality control strains: 1 strain in total, namely Escherichia coli ATCC25922, source of strains: purchased from Beina Chuanglian Biotechnology Co., Ltd. in the mall.

[0220] (2) Culture conditions: MHA medium, incubate at 35-37°C for 24h.

[0221] (3) Bacterial solution preparation: Before the test, each strain of bacteria was separated and purified by marking a single colony on an agar plate, and after culturing at 35-37°C, a single colony was picked and adjusted to about 0.5 McFarland units (about 10 8 CFU / mL), and then dilute the suspension 100 times to make the final concentra...

Embodiment 3

[0228] Example 3 Determination of the inhibitory activity of aryl ketone peptide deformylase inhibitors (compounds 1-22) on tumor cells

[0229]Wherein, the tumor refers to human colorectal cancer cells, human breast cancer cells, human non-small cell lung cancer cells, and human osteosarcoma cells. (See Table 3 for a list of compounds 1-22's tumor suppressor activity)

[0230] (1) Tumor cells used in the test: human osteosarcoma cells (Sjsa-1) (purchased from Guangzhou Saiku Biotechnology Co., Ltd.), human colon cancer cells (HCT116) (purchased from Guangzhou Saiku Biotechnology Co., Ltd.), human non- Small cell lung cancer cells (A549) (purchased from Guangzhou Saiku Biotechnology Co., Ltd.), human breast cancer cells (MCF-7) (purchased from Wuhan Punuosai Life Technology Co., Ltd.).

[0231] (2) Test method: CCK-8 method was used to determine the effect of aryl ketone peptide deformylase inhibitor (compound 1-22) on human osteosarcoma cells, human colon cancer cells, human...

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Abstract

The invention belongs to the technical field of antibacterial and anti-cancer drugs, and particularly relates to an aryl ketone peptide deformylase inhibitor and application thereof in antibacterial and anti-tumor aspects. The aryl ketone peptide deformylase inhibitor is novel in structure, better in activity and small in toxicity; on one hand, the aryl ketone peptide deformylase inhibitor has better antibacterial activity, especially on gram-negative bacteria (such as acinetobacter baumannii and the like), and can be applied to preparation of drugs for inhibiting pathogenic microorganisms; and on the other hand, the inhibitor has good anti-tumor activity, shows good inhibitory activity on various tumor cells (such as colorectal cancer, breast cancer, lung cancer and osteosarcoma), and can be applied to preparation of anti-tumor drugs. The aryl ketone peptide deformylase inhibitor has good application prospects in the antibacterial and anti-tumor aspects.

Description

technical field [0001] The invention belongs to the technical field of antibacterial and anticancer drugs, and in particular relates to an aryl ketone peptide deformylase inhibitor and its application in antibacterial and antitumor aspects. Background technique [0002] In recent years, due to the widespread use and abuse of antibiotics, many pathogenic microorganisms have developed severe resistance to existing antibiotics. The emergence of bacterial drug resistance, especially the multidrug resistance of Gram-negative bacteria, poses a huge threat to human life and health. Therefore, human beings urgently need to solve the above problems. The emergence of drug resistance in bacteria will lead to the reduction or even failure of the original antibiotics of certain types or mechanisms of action. One of the effective ways to solve the emergence of bacterial resistance is to develop antibacterial drugs with new mechanisms of action. It can be seen that finding new antibacteri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/54C07D401/06C07D417/06C07D401/10A61P31/04A61P35/00A61K31/403A61K31/5377A61K31/4439A61K31/427
CPCC07D209/54C07D401/06C07D417/06C07D401/10A61P31/04A61P35/00C07B2200/07
Inventor 钱宇胡吉迪石茂清黄佳武张芷菁史滔达徐新芳胡文浩
Owner SUN YAT SEN UNIV
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