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Novel compounds as Anti-mycobacterials

A technology of compounds and solvates, applied in the field of antibacterial compounds, can solve problems such as toxicity

Inactive Publication Date: 2019-10-01
THE UNIV OF SYDNEY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to potential toxicity concerns, these drugs are used only as a last resort

Method used

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  • Novel compounds as Anti-mycobacterials
  • Novel compounds as Anti-mycobacterials
  • Novel compounds as Anti-mycobacterials

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0227] 1. Materials and Methods

[0228] Analytical thin layer chromatography (TLC) was performed on commercially prepared silica plates (Merck Kieselgel 60 0.25 mm F254). Flash column chromatography was performed using 230-400 mesh Kieselgel 60 silica, eluting with distilled solvent as described. The proportions of solvents used for TLC and column chromatography are expressed in v / v. Compounds were visualized by UV light at 254 nm or stained with vanillin or cerium molybdate. Commercial materials were used as is unless otherwise stated. DCM and MeOH were distilled from calcium hydride, THF and diethyl ether were distilled from sodium / benzophenone. tert-butanol Before use, in the activated Dry over molecular sieves for at least 24 hours. Anhydrous DMF was purchased from Sigma Aldrich.

[0229] Device Information

[0230] Unless otherwise stated, at frequencies of 300.2, 400.2, 500.2 and 600.2 MHz, at 300 K, using BrukerAvance DPX 300, DPX 400, DPX 500 and DPX 600 NMR s...

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PUM

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Abstract

The present disclosure relates to antibacterial compounds. In particular, the compounds are for inhibiting the growth of bacteria, particularly Mycobacterium tuberculosis (Mtb), and / or targeting bacteria having phospho-MurNAc-pentapeptide translocase. The present disclosure also relates to compositions containing these compounds and methods of the use of these compounds and compositions.

Description

technical field [0001] The present invention relates to antimicrobial compounds. In particular, the compounds of the invention are useful for inhibiting the growth of bacteria, especially Mycobacterium tuberculosis (Mtb), and / or targeting bacteria with phospho-MurNAc-pentapeptide translocase . The invention also relates to compositions containing these compounds and methods of using these compounds and compositions. Background technique [0002] Tuberculosis (TB) is caused by infection with the bacterium Mycobacterium tuberculosis (Mtb). Tuberculosis has killed 1.5 million people, with 9.6 million new cases in 2014, according to the World Health Organization. [0003] Current treatment for TB is a six-month quadruple therapy of rifampicin, isoniazid, ethambutol, and pyrazinamide. This therapy provides an exceptional cure rate of over 95% for drug-sensitive TB, however, it is ineffective against multidrug-resistant (MDR) and extensively drug-resistant (XDR) TB. This is a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/037A61K38/04A61K38/07A61P11/00A61P31/04A61P31/06A61P31/08
CPCA61P31/04A61P31/06A61P11/00A61P31/08A61K38/00C07K5/0217C07K5/0215
Inventor R·J·佩恩W·J·布里顿A·特兰W·特兰
Owner THE UNIV OF SYDNEY
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