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Octahydrofuran [2, 3-b] pyridine-4, 6-diol and preparation method and application thereof

A technology of octahydrofuran and 3-b, which is applied in the field of octahydrofuran[2,3-b]pyridine-4,6-diol and its preparation, and can solve problems such as drug-resistant bacteria

Active Publication Date: 2021-08-06
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, clinical antibiotics mainly achieve bactericidal effect by inhibiting the function of TPase, such as penicillin, cephalosporin, monobactamycin, ceftaroline, ceftodol, carbapenem, etc., but these act on the TPase functional domain Corresponding drug-resistant bacteria appear in clinical practice
However, moenomycin, which targets TGase to exert antibacterial effects, has been used in animal feeding for decades without drug resistance

Method used

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  • Octahydrofuran [2, 3-b] pyridine-4, 6-diol and preparation method and application thereof
  • Octahydrofuran [2, 3-b] pyridine-4, 6-diol and preparation method and application thereof
  • Octahydrofuran [2, 3-b] pyridine-4, 6-diol and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation and separation of octahydrofuro[2,3-b]pyridine-4,6-diol

[0029] 1. Microbial fermentation

[0030] Preparation of seed solution: Take 3g of sea salt, 1.5g of malt extract powder, 100mL of water, and shake well. At 121°C, autoclave for 20 minutes, let it cool down, and use it as a seed medium. The strain Epicoccum sorghinum GXIMD02001 was inoculated in the seed medium in a biological safety cabinet and sealed. It was cultured at 25° C. and 180 rpm for 72 hours as a seed solution.

[0031] Large-scale fermentation: Weigh 150g of rice and put it into a 1000mL Erlenmeyer flask, add 150mL of water containing an appropriate amount of sea salt, seal and shake well. Autoclave at 121°C for 20 minutes. After taking it out and letting it cool, add 10mL of seed solution. Ferment at 25°C for 25-40 days.

[0032] 2. Obtaining the extract

[0033] Crush and mix the fermented rice culture medium, add ethyl acetate for ultrasonic extraction 3 times, filter...

Embodiment 2

[0040] Example 2: Octahydrofuro[2,3-b]pyridine-4,6-diol inhibits glycosyltransferase (TGase) activity

[0041]Liposome II analogs (5 μM) containing dimethylaminoazobenzoyl and coumarin groups, N-acetylmurazyme (1 μg / μL), different concentrations of compounds (0, 2.5, 5, 10, 20, 30, 40 μM) were mixed in the buffer, and after adding Clostridium PBP (5 μg / mL), cultured at 37°C and 80% humidity for 2 hours, using an excitation wavelength of 355nm and an emission wavelength of 460nm to detect once every 2min Fluorescence concentration. Buffer was used in place of the liposome II analog in negative control experiments. The strength of competitive inhibition is represented by the inhibition constant Ki. The results are shown in Table 2. Octahydrofuro[2,3-b]pyridine-4,6-diol has a certain inhibitory effect on glycosyltransferase.

[0042] The inhibition constant of table 2 compound to glycosyltransferase

[0043]

Embodiment 3

[0044] Example 3: Octahydrofuro[2,3-b]pyridine-4,6-diol antibacterial activity

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Abstract

The invention discloses octahydrofuran [2, 3-b] pyridine-4, 6-diol and a preparation method and application thereof. The octahydrofuran [2, 3-b] pyridine-4, 6-diol can inhibit the activity of glycosyl transferase (TGase), has a certain inhibiting effect on staphylococcus aureus, escherichia coli, bacillus subtilis, acinetobacter baumannii, klebsiella pneumoniae and methicillin-resistant staphylococcus aureus, and can be used for preparing a medicine for preventing and treating diseases. The compound can be used for preparing antibacterial drugs, and provides a candidate compound for new antibacterial drugs. According to the preparation method, the compound is obtained by carrying out compound separation on a culture medium obtained after fermentation of a marine-derived fungus Epicoccum soghrinum GXIMD02001. Compared with a traditional chemical synthesis method, the method has the advantages of being environmentally friendly and high in efficiency.

Description

technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and specifically relates to octahydrofuro[2,3-b]pyridine-4,6-diol and its preparation method and application. Background technique [0002] With the continuous increase of bacterial resistance and the depletion of terrestrial resources, antibiotics from terrestrial biological sources can no longer meet the needs of human health. In order to discover antibiotic lead compounds with significant activity and specific targets and reduce the chance of repeated research, people have gradually turned their attention to marine biological resources that are in a unique ecological environment, have many secondary metabolites, are novel, and are still underdeveloped. Hilary D. Marston et al pointed out that discovering new antibiotic drugs in unexploited marine natural products is an important way to solve antibiotic resistance (Journal of the American Medical Association, 2016, 316(11): 1193-1204...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/048A61P31/04C12P17/18C12R1/645
CPCC07D491/048A61P31/04C12P17/18Y02A50/30
Inventor 陈显强邢楠楠刘永宏高程海
Owner GUANGXI UNIV OF CHINESE MEDICINE