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Structural modification of 8-methoxy psoralen and its preparation method and application

A technology of structural formula and inhibitory effect, applied in the field of structural modification of natural compounds, can solve the problems of antibiotic abuse, drug-resistant drugs, residues, etc.

Active Publication Date: 2020-06-16
BEIJING UNIV OF AGRI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main treatment method is the use of antibiotics. However, the use or even abuse of a large number of antibiotics has brought serious problems such as drug resistance and drug residues.

Method used

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  • Structural modification of 8-methoxy psoralen and its preparation method and application
  • Structural modification of 8-methoxy psoralen and its preparation method and application
  • Structural modification of 8-methoxy psoralen and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、8

[0076] The preparation of the structural modifier of embodiment 1,8-methoxy psoralen

[0077] The present invention modifies the A, B, and C tricyclic structures of the 8-methoxypsoralen parent skeleton of formula M, and the modified active sites are mainly concentrated on C-6, C-, and C- of the A ring (furan ring). The 7-position and the C-8 and C-5 positions of the B ring (benzene ring).

[0078]

[0079] The structural modification of 8-methoxypsoralen is mainly divided into three parts.

[0080] The first part is the structural modification of the C-5 and C-8 positions of the B ring (benzene ring). Under the action of boron tribromide, the methoxy group of 8-methoxy psoralen is removed to generate hydroxyl group. The entire reaction time is about 4 hours. After quenching, extraction, concentration and drying, a large amount of yellow solid is obtained, and the yield is about 82%. Using 8-hydroxy psoralen as a substrate, under alkaline conditions (such as sodium carbo...

Embodiment 2、8

[0188] The bacteriostatic activity of the structural modification of embodiment 2, 8-methoxypsoralen to enterotoxigenic Escherichia coli

[0189] In this experiment, the structural modification of 8-methoxypsoralen synthesized in Example 1 was measured by constant broth double dilution method to determine its minimum inhibitory concentration (MIC value) for in vitro antibacterial effect on enterotoxigenic Escherichia coli evaluation of. The antibacterial rate was calculated by comparing the positive control without antibiotics.

[0190] 1. Materials and methods

[0191] 1.1 Experimental materials

[0192] 1.1.1 Tested strains

[0193] The enterotoxigenic Escherichia coli in this example is enterotoxigenic Escherichia coli (ETEC) F4ac, provided by the School of Animal Science and Technology, China Agricultural University (identification and analysis of piglet enterotoxigenic Escherichia coli (ETEC) F4ac receptor gene Functional verification. Wang Wenwen. Doctoral dissertati...

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Abstract

The invention discloses a structural modifier of 8-methoxypsoralen as well as a preparation method and application of the . The structural modifier of the 8-methoxypsoralen provided by the invention is a compound B20 shown as a formula 1 or a compound A10 shown as a formula 2. The bacteriostatic activity of the compound B20 for enterotoxigenic escherichia coli at the concentration of 64 mu g / mL is2.3 times of that of the 8-methoxypsoralen; the bacteriostatic activity of the compound A10 for enterotoxigenic escherichia coli at the concentration of 64 mu g / mL is 2.4 times of the 8-methoxypsoralen. The compound B20 and the compound A10 can be applied to the preparation of a medicament for treating and / or preventing piglet diarrhea. The formula 1 and the formula 2 are shown in the description.

Description

technical field [0001] The invention relates to a structural modification of 8-methoxy psoralen in the field of structural modification of natural compounds, a preparation method and application thereof. Background technique [0002] Piglet diarrhea is one of the frequently-occurring diseases in pig breeding, which has a great impact on the growth of pigs. Many breeding factories have no effective treatment methods, resulting in slow growth of piglets, and some even cause a large number of deaths, resulting in huge economic losses. Among the many pathogens causing diarrhea in piglets, enterotoxigenic Escherichia.coli (ETEC) is the main pathogenic factor causing diarrhea in piglets. At present, the main treatment method is the use of antibiotics. However, the use or even abuse of a large number of antibiotics has brought serious problems such as drug resistance and drug residues. Discovering biological activities from biosynthesized natural substances and using them as lead ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/366A61P31/04A61P1/12
CPCA23K20/126C07D493/04
Inventor 柳春梅赵莹李兵王赛朱慧泽孙雨
Owner BEIJING UNIV OF AGRI