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An eight-membered cyclic diene compound containing an amino group and a carboxyl group and its application

A cyclic diene and compound technology, applied in the field of new eight-membered cyclic diene compounds, can solve problems such as no antibacterial activity, and achieve the effects of obvious inhibitory effect, wide application range and strong antibacterial activity

Inactive Publication Date: 2015-12-09
FUJIAN AGRI & FORESTRY UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Substances close to the compound structural formula of the present invention, such as the substance Phenylephrine reported by Malakar, is a kind of anti-shock vasoactive drug, which is clinically used for infection, toxicity, anaphylactic shock, supraventricular tachycardia, prevention and treatment of general anesthesia and lumbar Hypotension during anesthesia, the structural formula is as (I); Padwa et al. obtain the substance Pentanoic acidfuran-2-ylamide through chemical synthesis, the structural formula is as (II); Wazeer et al. obtain the substance N-p-Methoxybenzyl-N-methylhydroxylamine through chemical synthesis, the structural formula is as (Ⅲ ); These structural formulas are characterized by having hydroxyl, amino, benzene ring or furan ring, but there is no relevant report on antibacterial activity

Method used

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  • An eight-membered cyclic diene compound containing an amino group and a carboxyl group and its application
  • An eight-membered cyclic diene compound containing an amino group and a carboxyl group and its application
  • An eight-membered cyclic diene compound containing an amino group and a carboxyl group and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: A new eight-membered cyclodiene compound containing amino and carboxyl groups

[0029] A new eight-membered ring diene compound containing amino and carboxyl groups, (2E,6Z)-2-amino-2,6-dienecarboxylic acid, its molecular structure is shown in (IV);

[0030]

Embodiment 2

[0031] Example 2: A preparation method of a new eight-membered cyclodiene compound containing amino and carboxyl groups

[0032] A preparation method of a new eight-membered ring diene compound containing an amino group and a carboxyl group, comprising the following steps:

[0033] 1. Fermentation broth preparation

[0034] Js-1 T After the strain was inoculated on PDA slant medium and cultured at 28°C for 7 days, the spores were scraped and inoculated in 100mL PDA liquid, and cultured at 28°C with 180r / min shaking for 48h, which was the seed medium; 5mL seed medium was inoculated into 100mL liquid fermentation medium (maltose 15g, glucose 10g, starch 5g, yeast powder 5g, KNO 3 2g, MgSO 4 0.5g, K 2 HPO 4 1g, NaCl0.5g, water 1000mL, pH7.0;), 28°C, 180r / min shaking culture for 6 days, the culture solution was centrifuged at 8000r / min for 10min, and the supernatant was Streptomyces Js-1 T of fermentation broth.

[0035] 2. Separation and purification

[0036] (a) Fermenta...

Embodiment 3

[0069] Embodiment 3, a kind of new eight-membered ring diene compound (C containing amino and carboxyl) 9 h 13 NO 2 )the use of

[0070] C 9 h 13 NO 2 The bacteriostasis rates to harmful Verrucospora, Phomopsis, Aspergillus niger, and longan scorch rot pathogens were 100%, 92.78%, 80.56%, and 58.33%, respectively. The specific bacteriostasis test methods are as follows:

[0071] Determination of fungal growth inhibitory activity adopts poisoned plate assay method, and the C prepared into 5mg / mL is taken 9 h 13 NO 2 Mother liquor, add the mother liquor to the solid PDA medium with a temperature of 50°C to obtain a poisoned medium with a final concentration of 25 μg / mL, mix it evenly and pour it into a flat plate, and inoculate the test medium with a diameter of 0.6cm after the medium is solidified. Bacteria cake of fungal pathogenic bacteria, with non-toxic medium as control. Cultivate at 25°C, measure the activity of the active substance by the growth rate method, tha...

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PUM

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Abstract

The invention relates to a new 8-membered ring diene compound containing amino and carboxyl and use thereof. The new 8-membered ring diene compound containing amino and carboxyl, (2E, 6Z)-2-amino-2, 6-diene carboxylic acid, has a molecular formula s C9H13NO2. The preparation method comprises preparation of the fermentation broth of the new 8-membered ring diene compound containing amino and carboxyl and separation purification. The new 8-membered ring diene compound containing amino and carboxyl provided by the invention has inhibitory effects on a variety of pathogenic fungi, especially has very obvious inhibition effects on harmful Mycogone perniciosa, Phomopsis and Aspergillus niger, and the inhibition rates are 100%, 92.78% and 80.56% respectively.

Description

technical field [0001] The present invention relates to a compound and its use, in particular to a new eight-membered ring diene compound containing an amino group and a carboxyl group and its use. Background technique [0002] Actinomycetes are an important source of microorganisms for natural products and drug development. According to statistics, among the more than 20,000 biologically active substances discovered so far, there are about 16,500 kinds of antibiotics and about 6,000 kinds of non-antibiotics, and more than half of the antibacterial active substances are from Actinomycetes produce, and antibiotics produced by Streptomyces account for more than 96% of the total antibiotics produced by actinomycetes. [0003] Substances close to the compound structural formula of the present invention, such as the substance Phenylephrine reported by Malakar, is a kind of anti-shock vasoactive drug, which is clinically used for infection, toxicity, anaphylactic shock, supraventr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C229/48C12P13/04A01P3/00C12R1/465
Inventor 温志强黄清铧
Owner FUJIAN AGRI & FORESTRY UNIV