Targeting DNA Gyrase to Combat Mycobacterium tuberculosis: An Update.
Aminocoumarins
Antibacterials
DNA gyrase
Fluoroquinolones
Mycobacterium tuberculosis
Pathogen.
Journal
Current topics in medicinal chemistry
ISSN: 1873-4294
Titre abrégé: Curr Top Med Chem
Pays: United Arab Emirates
ID NLM: 101119673
Informations de publication
Date de publication:
2019
2019
Historique:
received:
22
05
2018
revised:
10
10
2018
accepted:
02
01
2019
pubmed:
6
3
2019
medline:
11
7
2019
entrez:
6
3
2019
Statut:
ppublish
Résumé
DNA gyrase is a clinically validated drug target, currently targeted only by fluoroquinolone class of antibacterials. However, owing to increasing drug resistance as well as a concomitant reduction in the availability of newer classes of antibiotics, fluoroquinolones are increasingly being over-utilized in order to treat serious infections, including multi-drug resistant tuberculosis. This, in turn, increases the probability of resistance to fluoroquinolones, which is mediated by a single amino acid change in gyrA, leading to class-wide resistance. In this review, we provide an overview of the recent progress in identifying novel scaffolds which target DNA gyrase and provide an update on their discovery and development status.
Identifiants
pubmed: 30834837
pii: CTMC-EPUB-97034
doi: 10.2174/1568026619666190304130218
doi:
Substances chimiques
Antitubercular Agents
0
Topoisomerase II Inhibitors
0
DNA Gyrase
EC 5.99.1.3
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
579-593Informations de copyright
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