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Medical application of three carboxyl substituted aromatic compounds in treating pyrazinamide-resistance tuberculosis and tuberculosis

An aromatic compound, pyrazinamide-resistant technology, applied in the field of medicine, can solve the problems of inability to interact, POA to bind with RpsA, and inability to inhibit the trans-translation process, etc.

Inactive Publication Date: 2016-11-16
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, the PZA-resistant Mycobacterium tuberculosis produced clinically is partly due to the lack of pyrazinamidase (PZase), which prevents PZA from being hydrolyzed into the active form POA, and cannot bind to RpsA, resulting in the inability to inhibit the trans-translation process; Mainly due to the mutation of the RpsA structure, POA cannot combine with RpsA and cannot interact, resulting in inactivation

Method used

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  • Medical application of three carboxyl substituted aromatic compounds in treating pyrazinamide-resistance tuberculosis and tuberculosis
  • Medical application of three carboxyl substituted aromatic compounds in treating pyrazinamide-resistance tuberculosis and tuberculosis
  • Medical application of three carboxyl substituted aromatic compounds in treating pyrazinamide-resistance tuberculosis and tuberculosis

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Embodiment Construction

[0014] The present invention mainly relates to the discovery process of three types of carboxy-substituted aromatic compounds, as well as the research on the interaction between compounds and proteins at the molecular level (fluorescence quenching titration method), and the in vitro anti-tuberculosis Mycobacterium and anti-PZA-resistant Mycobacterium tuberculosis at the cellular level antibacterial experiment.

[0015] Drugs and Reagents

[0016] sample

[0017]

[0018] Reagents: control POA and PZA and compounds to be determined ZRL11, ZRL20 and ZRL15, ZRL25 and ZRL26; expressed and purified protein samples: MtRpsA (285-476), MtRpsAd438A (285-476) and MsRpsA (285-474); Mycobacterium strains: wild-type all-sensitive strains (H37Ra) and three clinically found PZA-resistant strains (PZA069, PZA080 and PZA073); other conventional chemical reagents: DMSO, D 2 O, phosphate buffer saline (PBS), etc.

[0019] Instruments: Fluorescence spectrophotometer (F-7000, Hitachi, Japan)...

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Abstract

The invention discloses three carboxyl substituted aromatic compounds (shown as Formulas (1-3)), which can antagonize ribosome proteins S1 (RpsA) of a ribosome 30S small subunit, effectively inhibit the growth of mycobacterium tuberculosis and pyrazinamide-resistance mycobacterium tuberculosis and can be used for preparing drugs for treating pyrazinamide-resistance tuberculosis and tuberculosis (as shown in Description).

Description

technical field [0001] The invention relates to the field of medicine, in particular to the medical application of three types of carboxy-substituted aromatic compound derivatives in pyrazinamide-resistant tuberculosis and tuberculosis treatment. Background technique [0002] Tuberculosis is one of the most prevalent diseases worldwide caused by Mycobacterium tuberculosis infection. Pyrazinamide (PZA) is the first-line anti-tuberculosis drug. It has obvious antibacterial effect on the slow-growing Mycobacterium tuberculosis in the acidic environment of phagocytic cells, and can effectively shorten the treatment cycle. It is currently the first-line anti-tuberculosis drug. The emergence of PZA-resistant Mycobacterium tuberculosis poses serious challenges to existing treatment options. The 2011 Science research results proposed the mechanism of action of PZA inhibiting the trans-translation of ribosomal protein S1 (RpsA) of the ribosomal 30S small subunit after being hydrolyz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61K31/404A61K31/4184A61K31/426A61K31/196A61P31/06
CPCA61K31/196A61K31/404A61K31/4184A61K31/426A61K31/505
Inventor 林克江支运宝仲艳雯
Owner CHINA PHARM UNIV
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