1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme inhibitor and preparation method thereof

An inhibitor and phosphorylation technology, which is applied in the preparation of carboxylic acid esters, chemical instruments and methods, botany equipment and methods, etc., can solve the problems of irrational clinical drug use and the reduction of clinical curative effect of antibiotics, and achieve the best DXR enzyme inhibition effect Effect

Inactive Publication Date: 2013-01-09
NORTHWEST UNIV
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Problems solved by technology

However, due to irrational clinical drug use and other reasons, new drug-resistant strains and drug-resistant mechanisms continue to emerge, making the clinical efficacy of antibiotics continue to decrease

Method used

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  • 1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme inhibitor and preparation method thereof
  • 1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme inhibitor and preparation method thereof
  • 1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme inhibitor and preparation method thereof

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Embodiment Construction

[0041] 1. Extraction, separation and structure identification of eugenol:

[0042] The compound eugenol mainly exists in the volatile oil of the dried flower buds of Syzygium aromaticum, a plant of the genus Syzygium in the family Oleaceae. Clove volatile oil was extracted by a general method to detect its DXR enzyme inhibitory activity, and it was found that it had weaker inhibitory activity. The volatile oil was divided into seven fractions with different polarities by silica gel column chromatography, and when the DXR enzyme inhibitory activity of each fraction was detected, it was found that the sixth fraction exhibited enhanced inhibitory activity, while the fifth and seventh fractions also showed weaker activity. activity. Further thin-layer chromatography analysis found that the sixth part presents a single uniform spot, and the fifth and seventh parts adjacent to it also contain this component. On this basis, it is preliminarily determined that the component in the si...

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Abstract

The invention discloses a 1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme inhibitor and a preparation method thereof. An essential oil ingredient of medicinal plant cloves is subjected to 1-deoxidation-D-xylulose5-phosphoric acid reduction isomerization enzyme (DXR) inhibitory activity detection, on the basis of a large quantity of theoretical analysis and experiments, the result that phenylpropanoids compound eugenol in the essential oil has good DXR enzyme inhibition activity is found out, thereby application of the eugenol and derivatives of the eugenol serving as a DXR enzyme inhibitor is determined, and further the eugenol and the derivatives of the eugenol with an excellent DXR enzyme inhibitory effect and the preparation method thereof are determined. Accordingly, the eugenol and the derivatives of the eugenol have a wide prospect for preparing antibiotic medicines or weedicides or immunomodulators.

Description

technical field [0001] The invention relates to a 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) inhibitor and a preparation method thereof. Background technique [0002] Antibiotics are currently the most widely used and most important drugs in clinical practice. Their application makes bacterial infection diseases well controlled and greatly reduces the morbidity and mortality of infectious diseases caused by pathogenic microorganisms. However, due to irrational clinical drug use and other reasons, new drug-resistant strains and drug-resistant mechanisms continue to emerge, making the clinical efficacy of antibiotics continue to decrease. The drug resistance of pathogenic microorganisms has become one of the biggest challenges in the field of medicine, and it is increasingly affecting doctors' choice of clinical drugs. It is of great practical significance to use new theories and newly established methods to find and develop some efficient and safe new antibiotics....

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/085A61K31/662A61K31/222A61K31/05A61K31/336A61K31/661A61P31/04A61P37/02A01N31/16A01N57/22A01N37/02A01N43/20A01N57/14A01P13/00C07F9/38C07C69/157C07C67/08C07C39/19C07C37/055C07D303/22C07D301/14C07F9/09
Inventor 高文运郝保华惠先李恒董磊
Owner NORTHWEST UNIV
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