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


Authors: Lun, S.; Guo, H.; Adamson, J.; Cisar, J. S.; Davis, T. D.; Chavadi, S. S.; Warren, J. D.; Quadri, L. E. N.; Tan, D. S.; Bishai, W. R.
Article Title: Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice
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] inhibitsM. 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 inhibitedM. tuberculosis growth in the mouse lung, providing the first in vivo proof of concept for this novel antibacterial strategy. Copyright © 2013, American Society for Microbiology. All Rights Reserved.
Journal Title: Antimicrobial Agents and Chemotherapy
Volume: 57
Issue: 10
ISSN: 0066-4804
Publisher: American Society for Microbiology  
Date Published: 2013-10-01
Start Page: 5138
End Page: 5140
Language: English
DOI: 10.1128/aac.00918-13
PROVIDER: scopus
PUBMED: 23856770
PMCID: PMC3811451
DOI/URL:
Notes: --- - "Export Date: 1 October 2013" - "CODEN: AMACC" - "Source: Scopus"
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  1. Derek S Tan
    91 Tan
  2. Justin Scott Cisar
    5 Cisar
  3. Tony Davis
    2 Davis