8‐Hydroxyquinolines are bactericidal against Mycobacterium tuberculosis

ABSTRACT There is an urgent need for new treatments effective against Mycobacterium tuberculosis, the causative agent of tuberculosis. The 8‐hydroxyquinoline series is a privileged scaffold with anticancer, antifungal, and antibacterial activities. We conducted a structure–activity relationship stud...

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Bibliographic Details
Published in:Drug development research 2019-08, Vol.80 (5), p.566-572
Main Authors: Odingo, Joshua O., Early, Julie V., Smith, Jake, Johnson, James, Bailey, Mai A., Files, Megan, Guzman, Junitta, Ollinger, Juliane, Korkegian, Aaron, Kumar, Anuradha, Ovechkina, Yulia, Parish, Tanya
Format: Article
Language:English
Subjects:
Analogs
Animals
antibacterial
Anticancer properties
Antitubercular agents
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Bactericidal activity
Chlorocebus aethiops
Cytotoxicity
Fungicides
Genomics
Hep G2 Cells
Humans
Hydroxyquinoline
Hydroxyquinolines - chemical synthesis
Hydroxyquinolines - chemistry
Hydroxyquinolines - pharmacology
Liability
Microbial Sensitivity Tests
Microbial Viability - drug effects
Minimum inhibitory concentration
Molecular Structure
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Mycobacterium tuberculosis - growth & development
Organic chemistry
Oxyquinoline - analogs & derivatives
Replication
Structure-Activity Relationship
Target recognition
Toxicity
Tuberculosis
Vero Cells
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Summary:ABSTRACT There is an urgent need for new treatments effective against Mycobacterium tuberculosis, the causative agent of tuberculosis. The 8‐hydroxyquinoline series is a privileged scaffold with anticancer, antifungal, and antibacterial activities. We conducted a structure–activity relationship study of the series regarding its antitubercular activity using 26 analogs. The 8‐hydroxyquinolines showed good activity against M. tuberculosis, with minimum inhibitory concentrations (MIC90) of 4 log kill at 10× MIC over 14 days. The majority of the compounds demonstrated cytotoxicity (IC50 of
ISSN:0272-4391
1098-2299
DOI:10.1002/ddr.21531