Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice Academic Article uri icon

Overview

MeSH Major

  • Anti-Bacterial Agents
  • Lung
  • Mycobacterium tuberculosis
  • Oxazoles

abstract

  • Mycobactin biosynthesis in Mycobacterium tuberculosis facilitates iron acquisition, which is required for growth and virulence. The mycobactin biosynthesis inhibitor salicyl-AMS [5'-O-(N-salicylsulfamoyl)adenosine] inhibits M. tuberculosis growth in vitro under iron-limited conditions. Here, we conducted a single-dose pharmacokinetic study and a monotherapy study of salicyl-AMS with mice. Intraperitoneal injection yielded much better pharmacokinetic parameter values than oral administration did. Monotherapy of salicyl-AMS at 5.6 or 16.7 mg/kg significantly inhibited M. tuberculosis growth in the mouse lung, providing the first in vivo proof of concept for this novel antibacterial strategy.

publication date

  • October 2013

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3811451

Digital Object Identifier (DOI)

  • 10.1128/AAC.00918-13

PubMed ID

  • 23856770

Additional Document Info

start page

  • 5138

end page

  • 40

volume

  • 57

number

  • 10