Preliminary pharmacokinetics of the bacterial virulence inhibitor N'-(3,5-dibromo-2-hydroxy-benzylidenene)-nicotinic acid hydrazide
2012 (English)In: Advances in Yersinia Research, Springer, 2012, 349-356 p.Chapter in book (Other academic)
Bacterial virulence inhibitors are potential novel drugs that may be used to treat infections. N′-(3,5-dibromo-2-hydroxy-benzylidene)-nicotinic acid hydrazide, ME0052, has been shown to inhibit type III secretion (T3S) and virulence in several Gram-negative enteric pathogens including Yersinia pseudotuberculosis. In vitro data suggest that ME0052 may be developed into drugs against bacterial gastroenteritis. Here we describe preliminary pharmacokinetics of ME0052 after intraperitoneal and subcutaneous administration in mice. The aim of this work was to identify suitable formulations and to determine pharmacokinetic parameters prior to testing in animal infection models. Peak plasma concentrations above the IC50 for virulence inhibition were achieved with high dose formulations and the elimination half-life was prolonged from 0.5 to 3.4 h using a poloxamer 407-based slow-release formulation.
Place, publisher, year, edition, pages
Springer, 2012. 349-356 p.
, Advances in Experimental Medicine and Biology, ISSN 0065-2598 ; 954
salicylidene acylhydrazide, pharmacokinetics, preclinical testing, sustained release formulations, anti-chlamydial activity
Medicinal Chemistry Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)
Research subject Pharmaceutical Microbiology; Pharmaceutics
IdentifiersURN: urn:nbn:se:umu:diva-40486DOI: 10.1007/978-1-4614-3561-7_42ISI: 000333327900043ISBN: 978-1-4614-3560-0ISBN: 978-1-4614-3561-7OAI: oai:DiVA.org:umu-40486DiVA: diva2:400151
Originally published in thesis in manuscript form with the title: "Preliminary pharmacokinetics of the bacterial virulence inhibitor 3,5-dibromo-2-hydroxy-benzylidene nicotinic acid hydrazide"2011-02-242011-02-232015-06-10Bibliographically approved