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

Tytuł:: Phenoxyalkylimidazoles with an oxadiazole moiety are subject to efflux in Mycobacterium tuberculosis.
Autorzy:: Thayer MB; TB Discovery Research, Infectious Disease Research Institute, Seattle, WA, United States of America.
Parish T; TB Discovery Research, Infectious Disease Research Institute, Seattle, WA, United States of America.; Center for Global Infectious Disease Research, Seattle Children's Research Institute, Seattle, WA, United States of America.
Źródło:: PloS one [PLoS One] 2021 Jan 22; Vol. 16 (1), pp. e0239353. Date of Electronic Publication: 2021 Jan 22 (Print Publication: 2021).
Typ publikacji:: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Język:: English
Imprint Name(s):: Original Publication: San Francisco, CA : Public Library of Science
MeSH Terms:: Mycobacterium tuberculosis/*drug effects
Oxadiazoles/*pharmacology
Phenols/*pharmacology
Antitubercular Agents/pharmacology ; Bacterial Proteins/drug effects ; Carbonyl Cyanide m-Chlorophenyl Hydrazone/metabolism ; Carbonyl Cyanide m-Chlorophenyl Hydrazone/pharmacology ; Humans ; Isoniazid/chemistry ; Isoniazid/pharmacology ; Membrane Transport Proteins/drug effects ; Microbial Sensitivity Tests/methods ; Oxadiazoles/chemistry ; Phenols/chemistry ; Reserpine/metabolism ; Reserpine/pharmacology
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Grant Information:: R01 AI099188 United States AI NIAID NIH HHS
Substance Nomenclature:: 0 (Antitubercular Agents)
0 (Bacterial Proteins)
0 (Membrane Transport Proteins)
0 (Oxadiazoles)
0 (Phenols)
555-60-2 (Carbonyl Cyanide m-Chlorophenyl Hydrazone)
8B1QWR724A (Reserpine)
V83O1VOZ8L (Isoniazid)
Entry Date(s):: Date Created: 20210122 Date Completed: 20210430 Latest Revision: 20210430
Update Code:: 20240105
PubMed Central ID:: PMC7822546
DOI:: 10.1371/journal.pone.0239353
PMID:: 33481781
: Czasopismo naukowe

Pełny tekst

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.
Competing Interests: The authors have declared that no competing interests exist.

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