NDLI: Fluoroquinolone action against clinical isolates of Mycobacterium tuberculosis: effects of a C-8 methoxyl group on survival in liquid media and in human macrophages.

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Fluoroquinolone action against clinical isolates of Mycobacterium tuberculosis: effects of a C-8 methoxyl group on survival in liquid media and in human macrophages.

Content Provider	Semantic Scholar
Author	Zhao, B. Y. Pine, Richard Domagala, John D. Drlica, Karl
Copyright Year	1999
Abstract	When the lethal action of a C-8 methoxyl fluoroquinolone against clinical isolates of Mycobacterium tuberculosis in liquid medium was measured, the compound was found to be three to four times more effective (as determined by measuring the 90% lethal dose) than a C-8-H control fluoroquinolone or ciprofloxacin against cells having a wild-type gyrA (gyrase) gene. Against ciprofloxacin-resistant strains, the C-8 methoxyl group enhanced lethality when alanine was replaced by valine at position 90 of the GyrA protein or when aspartic acid 94 was replaced by glycine, histidine, or tyrosine. During infection of a human macrophage model by wild-type Mycobacterium bovis BCG, the C-8 methoxyl group lowered survival 20- to 100-fold compared with the same concentration of a C-8-H fluoroquinolone. The C-8 methoxyl fluoroquinolone was also more effective than ciprofloxacin against a gyrA Asn94 mutant of M. bovis BCG. In an M. tuberculosis-macrophage system the C-8 methoxyl group improved fluoroquinolone action against both quinolone-susceptible and quinolone-resistant clinical isolates. Thus, a C-8 methoxyl group enhances the bactericidal activity of quinolones with N1-cyclopropyl substitutions; these data encourage further refinement of fluoroquinolones as antituberculosis agents.
Starting Page	1
Ending Page	5
Page Count	5
File Format	PDF HTM / HTML
Alternate Webpage(s)	http://aac.asm.org/content/43/3/661.full.pdf
PubMed reference number	10049284v1
Volume Number	43
Issue Number	3
Journal	Antimicrobial agents and chemotherapy
Language	English
Access Restriction	Open
Subject Keyword	Alanine Antitubercular Agents Aspartic Acid Bacillus Calmette-Guerin C-8 protein, Rhynchosciara americana Ciprofloxacin ELECTROSURGICAL DEVICE Fluoroquinolones Genus Mycobacterium Glycine Histidine Mycobacterium bovis Ag:PrThr:Pt:Bld:Ord Mycobacterium tuberculosis Quinolones Tyrosine Valine
Content Type	Text
Resource Type	Article

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