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Medical application of n-(thiophene-2)amide derivatives in pyrazinamide-resistant tuberculosis and tuberculosis treatment

A technology resistant to pyrazinamide and amide compounds, applied in the field of medicine, can solve the problems of inability to interact, inability of POA to combine with RpsA, inability to inhibit trans-translation process, etc.

Inactive Publication Date: 2019-07-09
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 n-(thiophene-2)amide derivatives in pyrazinamide-resistant tuberculosis and tuberculosis treatment

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Embodiment Construction

[0013] The present invention mainly relates to the discovery process of compounds containing N-(thiophene-2) amides, and the research on the interaction between compounds and proteins at the molecular level (fluorescence quenching titration method), and the in vitro anti-mycobacterium tuberculosis and resistance to PZA at the cellular level Antibacterial test of Mycobacterium tuberculosis.

[0014] Drugs and Reagents

[0015] sample

[0016]

[0017] Reagents: control POA and PZA and compounds to be determined ZRL07 and 08; expressed and purified protein samples: MtRpsA (285-476), MtRpsAd438A (285-476) and MsRpsA (285-474); Mycobacterium tuberculosis strain: wild type All-sensitive strains (H37Ra) and 3 clinically found PZA-resistant strains (PZA069, PZA080 and PZA073); other conventional chemical reagents: DMSO, D 2 O, phosphate buffer saline (PBS), etc.

[0018] Instruments: Fluorescence spectrophotometer (F-7000, Hitachi, Japan), Roche culture medium, constant tempera...

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Abstract

The present invention discloses ribosomal protein S1(RpsA) with structural N-(thiophene-2)amide derivatives (formula (1)) antagonistic ribosome 30S small subunits, and the protein can effectively inhibit the growth of Mycobacterium tuberculosis and pyrazinamide-resistant Mycobacterium tuberculosis and can be used to prepare drugs for treating pyrazinamide-resistant tuberculosis and tuberculosis.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the medical application of N-(thiophene-2) amide derivatives in the treatment of pyrazinamide-resistant tuberculosis and tuberculosis. 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 hydrolyzed into pyrazinoic acid ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D285/135C07D277/46A61K31/426A61K31/433A61P31/06
CPCC07D277/46C07D285/135
Inventor 林克江支运宝陈萍萍
Owner CHINA PHARM UNIV
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