A kind of purposes of rifamycin-nitroimidazole coupling molecule

A technology of nitroimidazolium and rifamycin, which is applied in the field of medicinal chemistry, can solve the problems of weak antibacterial activity and achieve strong antibacterial effect and strong antibacterial activity

Active Publication Date: 2017-11-07
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, from its structure-activity relationship and theoretical speculation, its activity against rifamycin and metronidazole double-resistant strains should be comparable to that of a 1:1 molar ratio mixture of rifamycin (rifampicin) and metronidazole , no or only weak antibacterial activity

Method used

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  • A kind of purposes of rifamycin-nitroimidazole coupling molecule
  • A kind of purposes of rifamycin-nitroimidazole coupling molecule
  • A kind of purposes of rifamycin-nitroimidazole coupling molecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Antibacterial activity of a rifamycin-nitroimidazole conjugate molecule against Helicobacter pylori

[0019] 1.1 Materials and methods

[0020] 1.1.1 Selection of strains

[0021] ATCC#700392 (CB1531) is a wild-type strain, purchased from American Type Culture Collection (ATCC, Manassas, Virginia). CB1573, CB1609, CB1610, CB1612, CB1613, CB1614, CB1771, CB1893, CB1894, CB1900, CB1901, CB1902, CB1903, CB1993 are isogenic mutant strains obtained from CB1531 and carry specific drug resistance genes. Medical supplies. See Table 1 for strain description.

[0022] Table 1 The following strains derived from glycerol stock solution were inoculated on TSAII medium without drugs

[0023]

[0024] 1.1.2 Medium configuration

[0025] It was prepared in accordance with the Clinical Laboratory Standards Institute guideline (CLSI) M7-A7 (test method for determination of susceptibility of aerobic bacteria to antibiotics by dilution method, approved standard). The test substance was ...

Embodiment 2

[0047] Example 2 Antibacterial activity of a rifamycin-nitroimidazole conjugate molecule against the Gram-positive anaerobic toxigenic pathogen Clostridium difficile

[0048] 2.1 Materials and methods

[0049] 2.1.1 Selection of strains

[0050] ATCC#BAA-1382 (CB1921) is a toxin-producing Clostridium difficile, purchased from the American Type Culture Collection (ATCC, Manassas, Virginia). CB1934, CB1939, CB1940, CB1941, CB1942 are isogenic strains with specific resistance mutations obtained from CB1921. The test strains were all provided by Dannuo Medicine. See Table 4 for strain description. Table 4 The following strains derived from glycerol stock solution were inoculated on drug-free supplemental Brookfield agar medium

[0051]

[0052] * Note: CB1939 isogenic resistant strains have not been confirmed by sequencing, but CB1942 is a direct descendant of CB1939, indicating that at least there is

[0053] A mutation in gyrA (D71Y) or (T82A).

[0054] 2.1.2 Medium configuration

[00...

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Abstract

The invention discloses a new application of a rifamycin-nitroimidazole coupling molecule, which belongs to the field of medicinal chemistry. The rifamycin-nitroimidazole conjugate molecule of the present invention exhibits high activity to drug-resistant strains in the treatment of infection-related diseases such as Clostridium difficile and Helicobacter pylori, except for single-drug resistance to rifamycin Both bacteria and metronidazole mono-resistant bacteria have antibacterial activity, and have antibacterial effect on rifamycin and metronidazole double-resistant bacteria, and its activity is better than the 1:1 molar ratio combination of rifampicin and metronidazole.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and particularly relates to a new use of a rifamycin-nitroimidazole coupling molecule. Background technique [0002] The antibacterial compound 4-deoxy-3,4-[2-spiro-[2-(2-methyl-5-nitro-imidazol-1-yl) ethyl, which is in the research and development stage, is disclosed in US patent US 7,678,791 B2 Yl]-piperidin-4-yl]]-(1hydro)-imidazo-(2,5-dihydro)rifamycin S, namely rifamycin-nitroimidazole conjugate molecule, which is Both monomycin-resistant strains and metronidazole-resistant strains have antibacterial activity, indicating their dual-target characteristics. However, based on its structure-activity relationship and theoretical speculation, its activity against rifamycin and metronidazole resistant strains should be comparable to a 1:1 molar mixture of rifamycin (rifampicin) and metronidazole , No or only weak antibacterial activity. [0003] Rifamycin antibiotics are a class of antibiotics produc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/439A61P31/04
Inventor 马振坤格雷戈瑞·罗伯森
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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