Novel application of rifamycin-nitroimidazole coupling molecule

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

Active Publication Date: 2015-10-14
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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  • Novel application of rifamycin-nitroimidazole coupling molecule
  • Novel application of rifamycin-nitroimidazole coupling molecule
  • Novel application 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 the determination of the susceptibility of aerobic bacteria to antibiotics by the dilution method, approved standard). The test su...

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 there is at least one mutation in gyrA (D71Y) or (T82A).

[0053] 2.1.2 Medium configuration

[0054] It...

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Abstract

The present invention discloses a novel application of rifamycin-nitroimidazole coupling molecule and belongs to the field of medicinal chemistry. The rifamycin-nitroimidazole coupling molecule shows high activity to drug-resistant strains in the treatment of undistinguishable Clostridium, Helicobacter pylori infection related diseases, not only has antibacterial resistant activity to the rifamycin single drug-resistance bacteria and metronidazole single drug-resistance bacteria, but also has antibacterial activity against rifamycin resistant and metronidazole double drug-resistance bacteria; and the activity of the coupling molecule is superior to that of the composition of rifampicin and metronidazole in the molar ratio of 1:1.

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 Applications(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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