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A compound yt-011 against multi-drug resistant bacteria and its preparation method

A technology of multi-drug-resistant bacteria and compounds, applied in the field of antibiotics, to achieve the effect of broadening the discovery path, good reproducibility, and enriching research and development ideas

Active Publication Date: 2020-10-09
CHENGDU YATU BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, the situation of drug-resistant bacterial infections is becoming more and more serious. Although the World Health Organization (WHO) and governments of various countries have strengthened the rational use of antibiotics through various measures to slow down the further development of drug-resistant bacterial infections; In order to fundamentally solve the problem of drug-resistant bacterial infection, it is necessary to continuously develop new varieties of drugs against drug-resistant bacteria

Method used

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  • A compound yt-011 against multi-drug resistant bacteria and its preparation method
  • A compound yt-011 against multi-drug resistant bacteria and its preparation method
  • A compound yt-011 against multi-drug resistant bacteria and its preparation method

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Experimental program
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Effect test

Embodiment 1

[0020] Step 1: Inoculate A. teichomyceticus ATCC 31121 slant strain into the medium (0.5% glucose, 0.4% malt extract, 0.4% peptone, 0.1% yeast extract, 1% soybean powder, 0.25% NaCl , 0.5% CaCO 3 , 30mL / 250mL capacity), 28°C, 220rpm culture for about 48h, take the microbial culture solution to detect the glucose content, when the glucose content drops below 0.001%, add 2g of A40926 to the microbial culture solution to make the concentration in the culture solution 200μg / mL. Continue to cultivate, take samples regularly to detect the content of deacylated A40926, after deacylation is completed, adjust the pH to 11 with 1N sodium hydroxide, filter, concentrate the filtrate to 8ml, heat up to 60°C, add 12ml of acetone / isopropanol = 5 / 1 mixed solvent, lowered to room temperature, a solid precipitated, filtered and dried to obtain 1.1 g of deacylated A40926.

[0021] NMR (D 2 O,δ):

[0022] 2.91~2.93(1H,m),3.17~3.25(4H,m),3.30~3.53(4H,m),3.63~3.79(4H,m),3.90~3.93(1H,m),4.54~4.5...

Embodiment 2

[0032] Step 1: Inoculate A. teichomyceticus ATCC 31121 slant strain into the medium (0.5% glucose, 0.4% malt extract, 0.4% peptone, 0.1% yeast extract, 1% soybean powder, 0.25% NaCl , 0.5% CaCO 3 , 30mL / 250mL load), 28°C, 220rpm for about 48h, take the microbial culture solution to detect the glucose content, when the glucose content drops below 0.001%, add 4g of A40926 to the microbial culture solution to make the concentration in the culture solution 200μg / mL. Continue to cultivate, take samples regularly to detect the content of deacylated A40926, after deacylation is completed, adjust the pH to 11 with 1N sodium hydroxide, filter, concentrate the filtrate to 17ml, heat up to 60°C, add 25.5ml of acetone / isopropanol =5 / 1 mixed solvent, lowered to room temperature, a solid precipitated, filtered and dried to obtain 2.3 g of deacylated A40926.

[0033] Step 2: Add 20ml of methanol into a 50ml reaction bottle, add 2g of deacylated A40926 under stirring, open the external bath...

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Abstract

The invention discloses a compound YT-011 resisting multi-drug resistant bacteria and a preparation method thereof. The compound YT-011 has an important supporting effect on the discovery of drugs resisting drug resistant bacteria based on a pathogenic mechanism. A technology for preparing an antibacterial active substance having a novel structure through a structure-modified microorganism-derived active mother nucleus is used as a key technology. The compound YT-011 provides a feasible method for the discovery of the innovative drug. The microorganism-derived physiological active substance having structural diversity increases the discovery ways of innovative drugs, and enriches the research and development ideas.

Description

technical field [0001] The invention belongs to the field of antibiotics, and in particular relates to a compound YT-011 against multidrug-resistant bacteria and a preparation method thereof. Background technique [0002] Dalbavancin (Dalbavancin) intermediate A40926 is a glycopeptide substance discovered by scientists in 1984 when they cultivated and isolated Actinomadura from soil. In 2003, the producing bacteria of A40926 were classified as Nonomuraea genus Actinomycetes ATCC 39727 (Nonomuraea.sp ATCC 39727). [0003] At present, the situation of drug-resistant bacterial infections is becoming more and more serious. Although the World Health Organization (WHO) and governments of various countries have strengthened the rational use of antibiotics through various measures to slow down the further development of drug-resistant bacterial infections; but for patients infected with diseases, To fundamentally solve the problem of drug-resistant bacterial infection, it is necess...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00C12P21/02C07K1/06
CPCC07K9/008C12P21/005
Inventor 朱辉王元桦田敏邓涛范雪涛张翠英易欣曹艳茹严华聪
Owner CHENGDU YATU BIOLOGICAL TECH
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