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Rifamycin-isoniazide hybrid drug and preparation method thereof

A technology of rifamycin and rifamycin sodium, applied in antibacterial drugs, organic chemistry and other directions, can solve the problems of complex post-processing, difficult production methods, etc., achieve in vitro stability, improve pharmaceutical and pharmacokinetic properties, Enhanced therapeutic effect

Inactive Publication Date: 2017-09-29
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation method of general hybrid drugs is more difficult, and the post-processing is more complicated.

Method used

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  • Rifamycin-isoniazide hybrid drug and preparation method thereof
  • Rifamycin-isoniazide hybrid drug and preparation method thereof
  • Rifamycin-isoniazide hybrid drug and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0027] Synthesis of oxazine rifamycin: put 1.00 g (0.0014 mol) of rifamycin sodium in a 100 mL three-necked bottle, add 20 mL of N,N-dimethylformamide to dissolve it, put it into a stirring magnet, and put it into a stirring magnet at room temperature. Stir for 30 minutes, after fully dissolving, add 0.072g concentrated sulfuric acid (95%) (0.0007mol) for acidification, stir at room temperature for 30 minutes, the reaction solution changes from dark blue to dark red, then heat up to 35-50 ° C, slowly Slowly add N,N-dimethylol tert-butylamine 0.352g (0.0026mol) dropwise, after the completion of dropping, the reaction solution changes from dark red to dark blue, and continue to keep the reaction for 2 hours (use thin-layer chromatography silica gel plate to track the reaction), After the reaction was completed, it was cooled to room temperature, 200 mL of an aqueous solution with 2 drops of glacial acetic acid added dropwise to the reaction solution, stirred intermittently, a lar...

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Abstract

The invention relates to a rifamycin-isoniazide hybrid drug and a preparation method thereof. The rifamycin-isoniazide hybrid drug is prepared according to the preparation method which comprises the following steps: acidizing rifamycin sodium and then generating cyclisation with N,N-dihydroxymethyl tertbutylamine, thereby compounding oxazine rifamycin, and then performing condensation reaction on the oxazine rifamycin, piperazine and isoniazide, thereby acquiring the rifamycin-isoniazide hybrid drug. The rifamycin-isoniazide hybrid drug prepared according to the invention is stable in vitro, is difficult to degrade, is free from biological activity and can be dosed at multiple target points. The hybrid drug has higher biological activity, sterilizing effect equivalent to that of rifampicin and wide development prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and relates to a rifamycin-isoniazide hybrid medicine and a preparation method thereof. Background technique [0002] Rifamycin was discovered by Italian LePetti Company in 1975. They obtained rifamycin antibiotics from Streptomyces mediterranean isolated from French soil, which are divided into five types: A, B, C, D and E. The main component is B, and rifamycin O, S, SV was later found in the fermentation broth that produced the strain. Rifamycin antibiotics have broad-spectrum antibacterial effects against gram-positive bacteria such as Mycobacterium tuberculosis, leprosy, streptococcus, pneumococcus, especially resistant rifamycin antibiotics Staphylococcus aureus. powerful. It is also effective against some gram-negative bacteria. It is often used in combination with other anti-tuberculosis drugs to treat various types of tuberculosis and severe infections caused by drug-resista...

Claims

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Application Information

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IPC IPC(8): C07D498/08A61K31/443A61P31/06
CPCC07D498/08
Inventor 祝宏丁娇彭薇杨昭张焕
Owner WUHAN INSTITUTE OF TECHNOLOGY
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