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Fluoroquinolone comprising 7-(3-amino-4-oximido)-1-piperidyl substitutional group and application of composition thereof

A fluoroquinolone, piperidinyl technology, applied to fluoroquinolone compounds, the application field in the treatment of tuberculosis

Inactive Publication Date: 2010-10-20
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, sparfloxacin has the strongest anti-TB activity, but its use is strictly restricted due to its obvious phototoxicity

Method used

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  • Fluoroquinolone comprising 7-(3-amino-4-oximido)-1-piperidyl substitutional group and application of composition thereof
  • Fluoroquinolone comprising 7-(3-amino-4-oximido)-1-piperidyl substitutional group and application of composition thereof
  • Fluoroquinolone comprising 7-(3-amino-4-oximido)-1-piperidyl substitutional group and application of composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] In vitro anti-mycobacterial activity test

[0019] The anti-tuberculosis activity of the compound shown in formula (I) or its medicinal salt, hydrate is by measuring its minimum inhibitory concentration (MIC, μ g / mL) to Mycobacterium tuberculosis standard strain H37Rv ATCC 27294 and clinical isolate 09710 ) to represent. In this trial, ciprofloxacin and moxifloxacin and the first-line anti-tuberculosis drug rifampicin were used as control drugs. The minimum inhibitory concentration was determined as follows: sterile 48-well plate (special microculture plate for rapid drug susceptibility of Mycobacterium tuberculosis), according to the design requirements of the drug susceptibility test, each well was added with 2 times concentration medium (improved Michaelis 7H9 liquid culture medium) base) diluted drug. Each compound was made into an initial solution of appropriate concentration, diluted with culture medium (2×) to double the concentration of each compound used, eac...

Embodiment 2

[0025] Oral acute toxicity test

[0026] In order to measure the oral acute toxicity of the compound represented by the formula (I) or its pharmaceutically acceptable salt, hydrate, it has been carried out acute toxicity test, will contain the compound represented by the formula (I) or its pharmaceutically acceptable salt of different concentrations, The solution of hydrate was orally given to male mice, and the dose was 0.1ml / 10g body weight. After 7 days, the amount of dead mice was counted respectively, and the median lethal dose (LD) of each compound was calculated by Bliss program. 50 ). The results are listed in Table 2.

[0027] Oral acute toxicity in mice of table 2 experimental compounds

[0028] experimental compound

LD 50 (mg / kg)

Formula (I) compound (R=CH 3 )

＞4000

Formula (I) compound (R=CH 3 )Hydrochloride

＞4000

Formula (I) compound (R=C 2 h 5 ) monohydrate

＞4000

[0029] Experimental result...

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Abstract

The invention relates to new application of a fluoroquinolone compound comprising a 7-(3-amino-4-oximido)-1-piperidyl substitutional group, in particular to application of 1-cyclopropyl-6-flurine-8-methoxyl-7-[(3-amino-4-methyl / ethyl oximido) piperidyl-1-group]-1,4-dihydro-4-oxo quinoline-3-carboxylic acid, or medicinal salt, hydrate and composition thereof in curing tuberculosis. Compared with the conventional clinic first-line antitubercular medicament (such as rifampicin) and a second-line antitubercular fluoroquinolones medicament (such as ciprofloxacin and the like), the fluoroquinolone compound has more excellent antitubercular mycobacteria activity.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a new application of a class of fluoroquinolone compounds with 7-(3-amino-4-oximino)-1-piperidinyl substituents. More specifically, the present invention relates to 1-cyclopropyl-6-fluoro-8-methoxy-7-[(3-amino-4-methyl / acetoximino)piperidin-1-yl]-1, Application of 4-dihydro-4-oxoquinoline-3-carboxylic acid or its medicinal salt, hydrate and composition in treating tuberculosis. Background technique [0002] Tuberculosis (TB) is one of the major infectious diseases caused by Mycobacterium tuberculosis (MTB), which seriously endangers human health. Since the 1980s, the incidence of drug-resistant TB, especially multi-drug-resistant TB (MDR-TB), has been increasing and the combination of TB and HIV / AIDS has caused the TB epidemic to rise again, becoming a major public health problem and a global concern. social problem. According to statistics, there are 8 million new TB patients ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/4709A61P31/06
Inventor 郭慧元刘明亮刘秉全胡锦生吴金韦王哲
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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