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Anti-tuberculous compound, application of compound to preparation of anti-tuberculous medicines and anti-tuberculous medicine composition

An anti-tuberculosis and compound technology, applied in the field of medicine, can solve the problems of no drugs available, lack of new anti-tuberculosis drugs, etc.

Inactive Publication Date: 2019-02-01
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is a shortage of new anti-tuberculosis drugs, and only two new drugs have been launched in the past fifty years. Once drug resistance spreads, it will fall into the dilemma of no drugs available

Method used

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  • Anti-tuberculous compound, application of compound to preparation of anti-tuberculous medicines and anti-tuberculous medicine composition
  • Anti-tuberculous compound, application of compound to preparation of anti-tuberculous medicines and anti-tuberculous medicine composition
  • Anti-tuberculous compound, application of compound to preparation of anti-tuberculous medicines and anti-tuberculous medicine composition

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Experimental program
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Effect test

preparation example Construction

[0049] The present invention has no special requirements on the preparation method of the dosage form described in the above scheme, and the anti-tuberculosis compound provided by the present invention can be prepared into a drug in a corresponding dosage form by using methods well known to those skilled in the art.

[0050] The anti-tuberculosis compound and anti-tuberculosis drug composition of the present invention can be used for preventing or treating tuberculosis in mammals (such as humans), and during the treatment or prevention process, a preventive or therapeutic effective amount of the present invention is given to a subject in need Provides anti-tuberculosis compounds. The anti-tuberculosis compound of the present invention can be used in pure form, or in the form of prodrug, or in the form of the anti-tuberculosis drug composition provided by the present invention. In specific embodiments of the present invention, the actual dosage level of the active ingredient (a...

Embodiment 1

[0056] 1) Synthesis of p-bromobenzohydrazide (intermediate 3)

[0057] In a 250mL three-necked flask, add p-bromobenzoic acid (10.0g, 49.75mmol) and 100mL tetrahydrofuran, then add N,N'-carbonyldiimidazole (10.45g, 64.68mmol), TLC monitors whether the raw material reaction is complete, after the reaction is completed , slowly dropwise added 80% hydrazine hydrate (4.93g, 78.77mmol), after the dropwise completion, stirred and reacted for about 6 hours. TLC monitors whether the reaction of raw materials is complete (developing solvent: petroleum ether / ethyl acetate 1:1). After completion of the reaction, cool to room temperature, concentrate under reduced pressure to remove most of the organic solvent, add about 30 mL of water, beat for a while at room temperature, filter with suction, and wash with water to obtain a white flaky solid. Recrystallized from 15 mL of absolute ethanol to obtain 9.09 g of a white solid of intermediate 3, with a yield of 85%. m.p.166~167℃, consistent...

Embodiment 2

[0070] The IMB-SDb8 and IMB-SDc9 prepared in Example 1 were tested in vitro for the inhibitory activity of Mycobacterium tuberculosis H37Rv, using the commonly used anti-tuberculosis drug isoniazid as a comparison, the steps are as follows:

[0071] The in vitro anti-tuberculosis activity of IMB-SDb8 and IMB-SDc9 was determined by the microplate double dilution method.

[0072] 1) Transplant the MTB H37Rv strain into 7H9 medium, and culture it statically at 37°C for 10 days;

[0073] 2) Dilute the bacterial solution with fresh culture medium until the CFU of the bacterial cells is about 1×10 5 a / ml;

[0074] 3) Add the diluted bacterial solution to a 96-well plate, 200 μL per well for the first column, and 100 μL per well for the rest;

[0075] 4) Add the compound to the wells in the first row to a final concentration of 32 μg / ml, and perform a two-fold dilution so that the final concentration of the compound is diluted from 32 μg / ml to 0.125 μg / ml. There are 11 gradients in...

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Abstract

The invention provides an anti-tuberculous compound with a structure as shown in a formula I. The compound is an s-triazolo-thiadiazole derivative (IMB-SDb8) when n in the formula I is equal to 0, andthe compound is an s-triazolo-thiadiazine derivative (IMB-SDc9) when n in the formula I is equal to 1. According to activity evaluation results in an embodiment, the compound IMB-SDb8 and IMB-SDc9 has definite anti-tuberculous bacillus activity and a wide application prospect in the aspect of preparation of anti-tuberculous medicines and is good in bioavailability and low in toxicity.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an anti-tuberculosis compound and its application in the preparation of anti-tuberculosis drugs and an anti-tuberculosis drug composition. Background technique [0002] Tuberculosis is a chronic infectious disease caused by Mycobacterium tuberculosis complex (Mycobacterium tuberculosis complex, referred to as Mycobacterium tuberculosis or Mycobacterium tuberculosis), which can affect multiple organ systems throughout the body. 80-90% of the total. It can also affect the liver, kidney, brain, lymph nodes and other organs. The Mycobacterium tuberculosis complex includes Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium africanum, and Mycobacterium microti, and it is mainly Mycobacterium tuberculosis that causes disease in humans. [0003] In recent years, with the continuous increase of single-drug resistance (SDR-MTB), multi-drug resistance (MDR-MTB) and extensivel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D513/04A61K31/549A61K31/433A61P31/06
CPCA61P31/06C07D513/04
Inventor 肖春玲王玉成李子强邓琪刘忆霜关艳蒙建州王菊仙张国宁朱梅王保国
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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