Quinoxaline‐based efflux pump inhibitors restore drug susceptibility in drug‐resistant nontuberculous mycobacteria

Abstract: Nontuberculous mycobacteria (NTM) comprise several ubiquitous, environmentally localized bacteria that may be responsible for serious human diseases. NTM‐associated pulmonary infections largely affect individuals with underlying respiratory disease or chronic disease and immunosuppressed patients. Mycobacterium simiae and M. abscessus are two NTMs responsible for lung disease in immunocompetent and immunocompromised individuals. In this study, two NTM strains were isolated from two patients admitted to an Italian hospital and were identified as M. simiae and M. abscessus. The two NTMs were tested for drug susceptibility against different antibiotics. To restore drug susceptibility, a new series of 2‐aryl‐3‐phenoxymethyl‐quinoxaline derivatives (QXs) was designed, synthesized, and investigated as efflux pump inhibitors (EPIs) against two clinical isolates of the above‐cited NTMs, evaluating how EPIs can influence the drug minimal inhibitory concentration values and, therefore, the activity. The different\ resistance levels tracked in the clinical strains were reduced by EPIs, and in several cases, the susceptibility was completely restored. QXs also resulted as potential chemical probes to be used in drug susceptibility tests to identify the resistance origin when detected.

Standort
Deutsche Nationalbibliothek Frankfurt am Main
Umfang
Online-Ressource
Sprache
Englisch

Erschienen in
Quinoxaline‐based efflux pump inhibitors restore drug susceptibility in drug‐resistant nontuberculous mycobacteria ; day:09 ; month:05 ; year:2022 ; extent:8
Archiv der Pharmazie ; (09.05.2022) (gesamt 8)

Urheber
Corona, Paola
Ibba, Roberta
Piras, Sandra
Molicotti, Paola
Bua, Alessandra
Carta, Antonio

DOI
10.1002/ardp.202100492
URN
urn:nbn:de:101:1-2022051015011249039401
Rechteinformation
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Letzte Aktualisierung
15.08.2025, 07:34 MESZ

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Beteiligte

  • Corona, Paola
  • Ibba, Roberta
  • Piras, Sandra
  • Molicotti, Paola
  • Bua, Alessandra
  • Carta, Antonio

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