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Phenylhydrazine fork-containing meta-dicarbonyl compound, preparation method and application thereof in inhibiting growth activity of candida albicans

A compound, dicarbonyl technology, applied in the field of inhibition of Candida albicans growth activity, can solve problems such as toxic and side effects, difficult to solve the problem of azole drug resistance, and achieve good inhibitory effect

Inactive Publication Date: 2015-04-01
HUAZHONG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the P45014DM genes in fungi and mammals have 35%-42% sequence homology, this will inevitably lead to some toxicity to mammalian cells when azole antifungal drugs work on fungi. side effect
It can be seen that the research and development of new antifungal drugs targeting the P450 protein, the target of existing antifungal drugs, not only cannot avoid the toxic and side effects of azole antifungal drugs, but also is difficult to solve the problem of drug resistance of azole drugs

Method used

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  • Phenylhydrazine fork-containing meta-dicarbonyl compound, preparation method and application thereof in inhibiting growth activity of candida albicans
  • Phenylhydrazine fork-containing meta-dicarbonyl compound, preparation method and application thereof in inhibiting growth activity of candida albicans
  • Phenylhydrazine fork-containing meta-dicarbonyl compound, preparation method and application thereof in inhibiting growth activity of candida albicans

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Experimental program
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Effect test

Embodiment 2

[0069] The 6 compounds synthesized above were tested for enzymosome inhibition of Candida albicans fructose 1,6-bisphosphate aldolase. Fructose-1,6-bisphosphate aldolase can reversibly decompose fructose-1,6-bisphosphate into dihydroxyacetone phosphate and glyceraldehyde-3-phosphate. Under the action of triose phosphate isomerase (TIM), dihydroxyacetone phosphate can be converted into glyceraldehyde-3-phosphate. Finally, glyceraldehyde-3-phosphate is converted into glycerol-3-phosphate under the action of glyceraldehyde-3-phosphate dehydrogenase (GPDH), and at the same time, two molecules of NADH (nicotinamide adenine dinucleotide) are converted into NAD+. In the experiment, triose phosphate isomerase (TIM) and glyceraldehyde-3-phosphate dehydrogenase (GPDH) were used as coupling enzymes, and fructose 1,6-bisphosphate aldolase was determined by measuring the change of NADH absorbance at 340nm activity, and then reflect the inhibitory efficiency of the above-mentioned 6 kinds ...

Embodiment 3

[0071] 1. In vitro antifungal activity test:

[0072] The minimal inhibitory concentration (minimal inhibitory concentration) of the compounds to be screened against Candida albicans was detected by the Broth Microdilution method recommended by the American Clinical Laboratory Standards Institute (CLSI) CLSI-M27A3 and M38A2 documents. concentration, MIC), for antifungal activity screening. The inhibitory effects of compounds I-1 to I-6 on Candida albicans are shown in Table 1.

[0073] Table 1 The compound of general formula I is to Candida albicans FBA-II and to the inhibition of Candida albicans activity

[0074]

[0075] compound R 1 R 2 R 3 R 4 R 5 R 6 I 50 (μM) Mic 80 (μM) I-1 Oh H NO 2 H CF 3 CF 3 1.03±0.11 42.87

[0076] I-2 Oh SO 3 h H NO 2 CF 3 CF 3 8.35±1.47 35.30 I-3 Oh H H COOH CF 3 C 2 h 5 o 26.90±1.7 45.96 I-4 Oh H H NO 2 CF 3 C 2 h 5 o 3.17±0....

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Abstract

The invention relates to a phenylhydrazine fork-containing meta-dicarbonyl compound, a preparation method and an application thereof in inhibiting growth activity of candida albicans. The phenylhydrazine fork-containing meta-dicarbonyl compound is characterized by comprising a structure shown by a general formula I in the description, wherein in the general formula I, R1 represents hydroxyl, R2, R3 and R4 represent hydrogen, nitryl and carboxyl or sulfonic acid group; the substituent groups represented by R2, R3 and R4 are same or different; R5 and R6 represent methyl, trifluoromethyl or oxethyl; and substituent groups represented by R5 and R6 are same or different. The phenylhydrazine fork-containing meta-dicarbonyl compound has a good effect of inhibiting fructose-1,6-diphosphate aldolase of candida albicans, and the minimum IC50 value of the compound can reach 0.22 micron; and the phenylhydrazine fork-containing meta-dicarbonyl compound has a good effect of inhibiting the candida albicans, and can be used as an effective ingredient of a candida albicans bactericide.

Description

technical field [0001] The invention relates to a series of compounds containing phenylhydrazinylidene meta-dicarbonyls, a preparation method and their application in inhibiting the growth activity of Candida albicans. Background technique [0002] Candida albicans is a normal flora in the oral cavity, throat, intestinal tract, and vaginal mucosa of the human body, but it is also a common clinical opportunistic pathogen. For those with low immunity (diabetes, malignant tumors, blood diseases, severe malnutrition, etc.), it can cause superficial or deep Candida infection, and severe cases can cause systemic infection, which is life-threatening. In recent years, due to the widespread use of immunosuppressants, broad-spectrum antibiotics, and corticosteroids, as well as the increase in infections in organ transplants, patients with malignant tumors, and patients with acquired immunodeficiency syndrome (AIDS), the incidence of invasive fungal infections has shown an upward trend...

Claims

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Application Information

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IPC IPC(8): C07C251/76A61K31/15A61K31/255A61K31/215A61P31/10C07C309/49C07C303/22
Inventor 万坚任彦亮韩新亚朱秀云祝帅华彭浩冯玲玲李定
Owner HUAZHONG NORMAL UNIV
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