Accumulation of TB-Active Compounds in Murine Organs Relevant to Infection by
decoquinate
liquid chromatography-tandem mass spectrometry
organ concentrations
phenoxazine
tuberculosis
tuberculosis chemotherapy
Journal
Frontiers in pharmacology
ISSN: 1663-9812
Titre abrégé: Front Pharmacol
Pays: Switzerland
ID NLM: 101548923
Informations de publication
Date de publication:
2020
2020
Historique:
received:
06
02
2020
accepted:
30
04
2020
entrez:
9
6
2020
pubmed:
9
6
2020
medline:
9
6
2020
Statut:
epublish
Résumé
Tuberculosis (TB), the leading cause of death due to an infectious agent, requires prolonged and costly drug treatments. With the rise in incidence of MDR and XDR TB, newer more efficacious treatments which are better able to permeate into the deeper recesses of the human lung where bacteria reside are urgently required. To this end, two new promising drug candidates, the decoquinate derivative RMB041 and the phenoxazine PhX1, were assessed for their abilities to permeate into specific murine organs. In particular, PhX1 permeation into the lungs and heart was notably efficient, as reflected in the high relative AUC values of 9669 ± 120.2 min/nmol/mg and 12450 ± 45.2 min/nmol/mg for lung and heart tissue, respectively. However, neither compound maintained a free concentration in the lung which exceeded the compound's respective MIC
Identifiants
pubmed: 32508649
doi: 10.3389/fphar.2020.00724
pmc: PMC7248252
doi:
Types de publication
Journal Article
Langues
eng
Pagination
724Informations de copyright
Copyright © 2020 Tanner, Haynes and Wiesner.
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