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Issue 11, 2016
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SAR and identification of 2-(quinolin-4-yloxy)acetamides as Mycobacterium tuberculosis cytochrome bc1 inhibitors

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Abstract

A previous phenotypic screen by GSK identified 2-(quinolin-4-yloxy)acetamides as potent growth inhibitors of Mycobacterium tuberculosis (Mtb). We report the results of a preliminary structure–activity relationship (SAR) study of the compound class which has yielded more potent inhibitors. An Mtb cytochrome bd oxidase deletion mutant (cydKO) was found to be hypersensitive to most members of the compound library, while strains carrying single-nucleotide polymorphisms of the qcrB gene, which encodes a subunit of the menaquinol cytochrome c oxidoreductase (bc1) complex, were resistant to the library. These results identify that the 2-(quinolin-4-yloxy)acetamide class of Mtb growth inhibitors can be added to the growing number of scaffolds that target the M. tuberculosis bc1 complex.

Graphical abstract: SAR and identification of 2-(quinolin-4-yloxy)acetamides as Mycobacterium tuberculosis cytochrome bc1 inhibitors

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Publication details

The article was received on 28 Apr 2016, accepted on 17 Aug 2016 and first published on 22 Aug 2016


Article type: Research Article
DOI: 10.1039/C6MD00236F
Citation: Med. Chem. Commun., 2016,7, 2122-2127
  • Open access: Creative Commons BY-NC license
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    SAR and identification of 2-(quinolin-4-yloxy)acetamides as Mycobacterium tuberculosis cytochrome bc1 inhibitors

    N. Phummarin, H. I. Boshoff, P. S. Tsang, J. Dalton, S. Wiles, C. E. Barry 3rd and B. R. Copp, Med. Chem. Commun., 2016, 7, 2122
    DOI: 10.1039/C6MD00236F

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