8-Hydroxyquinolines are bactericidal against Mycobacterium tuberculosis.
Animals
Antitubercular Agents
/ chemical synthesis
Chlorocebus aethiops
Hep G2 Cells
Humans
Hydroxyquinolines
/ chemical synthesis
Microbial Sensitivity Tests
Microbial Viability
/ drug effects
Molecular Structure
Mycobacterium tuberculosis
/ drug effects
Oxyquinoline
/ analogs & derivatives
Structure-Activity Relationship
Vero Cells
Mycobacterium tuberculosis
tuberculosis
antibacterial
hydroxyquinoline
structure-activity relationship
Journal
Drug development research
ISSN: 1098-2299
Titre abrégé: Drug Dev Res
Pays: United States
ID NLM: 8204468
Informations de publication
Date de publication:
08 2019
08 2019
Historique:
received:
10
12
2018
revised:
21
02
2019
accepted:
05
03
2019
pubmed:
21
3
2019
medline:
28
1
2020
entrez:
21
3
2019
Statut:
ppublish
Résumé
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 <5 μM for some analogs. Small substitutions at C5 resulted in the most potent activity. Substitutions at C2 generally decreased potency, although a sub-family of 2-styryl-substituted analogs retained activity. Representative compounds demonstrated bactericidal activity against replicating M. tuberculosis with >4 log kill at 10× MIC over 14 days. The majority of the compounds demonstrated cytotoxicity (IC
Identifiants
pubmed: 30893501
doi: 10.1002/ddr.21531
pmc: PMC6767403
doi:
Substances chimiques
Antitubercular Agents
0
Hydroxyquinolines
0
Oxyquinoline
5UTX5635HP
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
566-572Informations de copyright
© 2019 The Authors. Drug Development Research published by Wiley Periodicals, Inc.
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