Here another nice article regarding antibacterial properties and 8-HQs:
Antimicrob. Agents Chemother., 2016
8-Hydroxyquinolines are boosting-agents of copper related toxicity in Mycobacterium tuberculosis
Shah, S; Dalecki, AG; Malalasekera, AP; Crawford, CL; Michalek, SM; Kutsch, O; Sun, J; Bossmann, SH; Wolschendorf, F
Copper ions (Cu) are the most important immunological metal-related toxin implemented in controlling bacterial infection. Impairment of bacterial Cu resistance reduces viability within the host. Thus, pharmacologically enhancing Cu-mediated antibacterial toxicity may lead to novel strategies in drug discovery and development. Screening for Cu-toxicity enhancing antibacterial molecules identified 8-hydroxyquinoline (8HQ) as a potent Cu-dependent bactericidal inhibitor of Mycobacterium tuberculosis (Mtb). The minimal inhibitory concentration of 8HQ in the presence of Cu was 0.16 μM against replicating and non-replicating Mtb. We found 8HQ's activity dependent on the presence of extracellular Cu and was related to an increase in cell-associated labile Cu ions. Both findings are consistent with 8HQ acting as Cu ionophore. Accordingly, we identified the 1:1 complex of 8HQ and Cu as its active form, with Zn, Fe, or Mn, neither enhancing nor reducing its Cu-specific action. This is remarkable considering that the respective metal complexes have nearly identical structures and geometry. Finally, we found 8HQ to kill Mtb selectively within infected primary macrophages. Given the stark Cu-dependent nature of 8HQs activity, this is the first piece of evidence that Cu ions within macrophages may bestow antibacterial properties to a Cu-dependent inhibitor of Mtb. In conclusion, our findings highlight the metal binding abilities of the 8-hydroxyquinoline scaffold as a potential focus for future medicinal chemistry and highlight the potential of innate immunity-inspired screening platforms to reveal molecules with novel modes of action against Mtb.
Copyright © 2016, American Society for Microbiology. All Rights Reserved.
We only have a library of over 2000 of these patented.
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