Phenoxyalkylimidazoles with an oxadiazole moiety are subject to efflux in Mycobacterium tuberculosis

Mai B. Thayer; Tanya Parish

doi:10.1371/journal.pone.0239353

Phenoxyalkylimidazoles with an oxadiazole moiety are subject to efflux in Mycobacterium tuberculosis

Mai B. Thayer
, Tanya Parish

Infectious Disease Research Institute
Amgen Incorporated
Seattle Biomedical Research Institute

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

Abstract

The phenoxyalkylimidazoles (PAI) are an attractive chemical series with potent anti-tubercular activity targeting Mycobacterium tuberculosis respiration. Our aim was to determine if the PAI compounds are subject to efflux. Two analogs containing an oxadiazole had improved potency in the presence of the efflux inhibitors reserpine and carbonyl cyanide m-chlorophenylhydrazine, whereas the potency of analogs with a diazole was not affected.

Original language	English
Article number	e0239353
Journal	PLoS ONE
Volume	16
Issue number	1 January
DOIs	https://doi.org/10.1371/journal.pone.0239353
Publication status	Published - 22 Jan 2021
Externally published	Yes

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SDG 3 Good Health and Well-being

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10.1371/journal.pone.0239353Licence: CC BY

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abstract = "The phenoxyalkylimidazoles (PAI) are an attractive chemical series with potent anti-tubercular activity targeting Mycobacterium tuberculosis respiration. Our aim was to determine if the PAI compounds are subject to efflux. Two analogs containing an oxadiazole had improved potency in the presence of the efflux inhibitors reserpine and carbonyl cyanide m-chlorophenylhydrazine, whereas the potency of analogs with a diazole was not affected.",

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AB - The phenoxyalkylimidazoles (PAI) are an attractive chemical series with potent anti-tubercular activity targeting Mycobacterium tuberculosis respiration. Our aim was to determine if the PAI compounds are subject to efflux. Two analogs containing an oxadiazole had improved potency in the presence of the efflux inhibitors reserpine and carbonyl cyanide m-chlorophenylhydrazine, whereas the potency of analogs with a diazole was not affected.

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Phenoxyalkylimidazoles with an oxadiazole moiety are subject to efflux in Mycobacterium tuberculosis

Abstract

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