Literature DB >> 2113793

MICs and MBCs of Win 57273 against Mycobacterium avium and M. tuberculosis.

L B Heifets1, P J Lindholm-Levy.   

Abstract

A new quinolone, Win 57273 [1-cyclopropyl-7-(2,6-dimethyl-4-pyridinyl)-6-fluoro-1,4-dihydro-4-oxo-3 - quinolonecarboxylic acid], synthesized by Sterling Research Group, was tested in vitro against Mycobacterium tuberculosis and Mycobacterium avium strains. The broth-determined MICs of this agent ranged from 1.0 to 4.0 micrograms/ml for M. tuberculosis strains and from 0.25 to 8.0 micrograms/ml for M. avium strains. A distinctive feature of this agent, in comparison with ofloxacin and ciprofloxacin, is its substantially greater activity at the low pHs. For M. avium strains, the MICs of Win 57273 were 2.0 micrograms/ml or less for 54.5% of strains at pH 6.8 and 85.5% of strains at pH 5.0. Win 57273 was more active than ciprofloxacin against M. avium strains, and this difference was very substantial for all M. avium strains at pH 5.0. Taking into account that the predominant locations of these organisms in vivo are within the phagosomes and phagolysosomes of macrophages, i.e., in acidic environments at pH 5.0 or lower, the greater activity of Win 57273 at low pH makes this quinolone especially promising for M. avium infection. The bactericidal activity of Win 57273 for M. avium strains was the same as that of ciprofloxacin, with MBCs from 4.0 to 16.0 micrograms/ml.

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Year:  1990        PMID: 2113793      PMCID: PMC171689          DOI: 10.1128/AAC.34.5.770

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


  26 in total

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Journal:  Antimicrob Agents Chemother       Date:  1985-10       Impact factor: 5.191

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  9 in total

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2.  In vitro susceptibility of Mycobacterium avium complex to the new fluoroquinolone sparfloxacin (CI-978; AT-4140) and comparison with ciprofloxacin.

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Journal:  Antimicrob Agents Chemother       Date:  1990-12       Impact factor: 5.191

Review 3.  Antimicrobial agent resistance in mycobacteria: molecular genetic insights.

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4.  Cloning and nucleotide sequence of Mycobacterium tuberculosis gyrA and gyrB genes and detection of quinolone resistance mutations.

Authors:  H E Takiff; L Salazar; C Guerrero; W Philipp; W M Huang; B Kreiswirth; S T Cole; W R Jacobs; A Telenti
Journal:  Antimicrob Agents Chemother       Date:  1994-04       Impact factor: 5.191

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Authors:  Y Cohen; C Perronne; C Truffot-Pernot; J Grosset; J L Vilde; J J Pocidalo
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Authors:  M R Jacobs
Journal:  Drugs       Date:  1995       Impact factor: 9.546

9.  In vitro anti-Mycobacterium avium activities of quinolones: predicted active structures and mechanistic considerations.

Authors:  G Klopman; J Y Li; S Wang; A J Pearson; K Chang; M R Jacobs; S Bajaksouzian; J J Ellner
Journal:  Antimicrob Agents Chemother       Date:  1994-08       Impact factor: 5.191

  9 in total

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