Literature DB >> 20516287

In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.

Michael J Pucci1, Maria Ackerman, Jane A Thanassi, Carolyn M Shoen, Michael H Cynamon.   

Abstract

ACH-702 is a new isothiazoloquinolone with potent in vitro and in vivo activities against important bacterial pathogens, including Staphylococcus aureus. In this study, ACH-702 was found to have promising in vitro antibacterial activity against Mycobacterium tuberculosis, with MICs of <or=1 microg/ml, comparable to that of the fluoroquinolone moxifloxacin for quinolone-susceptible isolates but superior to that for quinolone-resistant isolates. Biochemical assays involving M. tuberculosis gyrase enzymes indicated that ACH-702 had significantly improved inhibitory activity compared with fluoroquinolones.

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Year:  2010        PMID： 20516287      PMCID： PMC2916342          DOI： 10.1128/AAC.00287-10

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  15 in total

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2.  Novel gyrase mutations in quinolone-resistant and -hypersusceptible clinical isolates of Mycobacterium tuberculosis: functional analysis of mutant enzymes.

Authors:  Alexandra Aubry; Nicolas Veziris; Emmanuelle Cambau; Chantal Truffot-Pernot; Vincent Jarlier; L Mark Fisher
Journal:  Antimicrob Agents Chemother       Date:  2006-01       Impact factor: 5.191

3.  Global trends in resistance to antituberculosis drugs. World Health Organization-International Union against Tuberculosis and Lung Disease Working Group on Anti-Tuberculosis Drug Resistance Surveillance.

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Journal:  N Engl J Med       Date:  2001-04-26       Impact factor: 91.245

4.  Emergence of Mycobacterium tuberculosis with extensive resistance to second-line drugs--worldwide, 2000-2004.

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5.  Sequence analyses of just four genes to detect extensively drug-resistant Mycobacterium tuberculosis strains in multidrug-resistant tuberculosis patients undergoing treatment.

Authors:  Silke Feuerriegel; Helen S Cox; Nana Zarkua; Hamraev A Karimovich; Kai Braker; Sabine Rüsch-Gerdes; Stefan Niemann
Journal:  Antimicrob Agents Chemother       Date:  2009-05-26       Impact factor: 5.191

6.  In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.

Authors:  Michael J Pucci; Jijun Cheng; Steven D Podos; Christy L Thoma; Jane A Thanassi; Douglas D Buechter; Gohar Mushtaq; Gerald A Vigliotti; Barton J Bradbury; Milind Deshpande
Journal:  Antimicrob Agents Chemother       Date:  2007-01-22       Impact factor: 5.191

7.  An improved expression plasmid for affinity purification of Staphylococcus aureus gyrase A subunit.

Authors:  Jacob Strahilevitz; Yoshikuni Onodera; David C Hooper
Journal:  Protein Expr Purif       Date:  2005-09-21       Impact factor: 1.650

8.  Cloning and primary structure of Staphylococcus aureus DNA topoisomerase IV: a primary target of fluoroquinolones.

Authors:  L Ferrero; B Cameron; B Manse; D Lagneaux; J Crouzet; A Famechon; F Blanche
Journal:  Mol Microbiol       Date:  1994-08       Impact factor: 3.501

9.  Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.

Authors:  Andrea Von Groll; Anandi Martin; Pontus Jureen; Sven Hoffner; Peter Vandamme; Françoise Portaels; Juan Carlos Palomino; Pedro Almeida da Silva
Journal:  Antimicrob Agents Chemother       Date:  2009-08-17       Impact factor: 5.191

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Journal:  Emerg Infect Dis       Date:  2007-03       Impact factor: 6.883
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Review 2.  Current prospects for the fluoroquinolones as first-line tuberculosis therapy.

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Journal:  Antimicrob Agents Chemother       Date:  2011-08-29       Impact factor: 5.191

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Journal:  Bioorg Med Chem Lett       Date:  2011-06-06       Impact factor: 2.823

4.  In vitro and in vivo profiles of ACH-702, an isothiazoloquinolone, against bacterial pathogens.

Authors:  Michael J Pucci; Steven D Podos; Jane A Thanassi; Melissa J Leggio; Barton J Bradbury; Milind Deshpande
Journal:  Antimicrob Agents Chemother       Date:  2011-04-04       Impact factor: 5.191

5.  The efflux pump inhibitor timcodar improves the potency of antimycobacterial agents.

Authors:  Trudy H Grossman; Carolyn M Shoen; Steven M Jones; Peter L Jones; Michael H Cynamon; Christopher P Locher
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6.  Crystal structure and stability of gyrase-fluoroquinolone cleaved complexes from Mycobacterium tuberculosis.

Authors:  Tim R Blower; Benjamin H Williamson; Robert J Kerns; James M Berger
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7.  New classes of alanine racemase inhibitors identified by high-throughput screening show antimicrobial activity against Mycobacterium tuberculosis.

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8.  Drug-resistant tuberculosis: emerging treatment options.

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Journal:  Clin Pharmacol       Date:  2011-12-14

Review 9.  New antibiotic agents in the pipeline and how they can help overcome microbial resistance.

Authors:  Ian M Gould; Abhijit M Bal
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  9 in total

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