Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0348321 (Haemophilus)
 15,372 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

DL-8280, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido-(1,2,3-de)1,4-benzoxazine-6-carboxylic acid, is a new nalidixic acid analog with a broad spectrum of antibacterial activity against gram-negative and gram-positive bacteria, including obligate anaerobes. The activity of DL-8280 against Enterobacteriaceae, Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria gonorrhoeae, and Clostridium perfringens was roughly comparable to that of norfloxacin and far exceeded that of pipemidic acid and nalidixic acid. DL-8280 had greater activity against Staphylococcus spp., Streptococcus spp., Pseudomonas maltophilia, Acinetobacter spp., and Bacteroides fragilis than did norfloxacin, pipemidic acid, and nalidixic acid. Nalidixic acid-resistant Enterobacteriaceae, ampicillin-resistant gonococci, and clindamycin-resistant obligate anaerobes were also susceptible to DL-8280. The activity of DL-8280 was affected very little by inoculum size, and its action was bactericidal at two times the minimal inhibitory concentrations at most. Administered orally to mice experimentally infected with Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis, Serratia marcescens, or P. aeruginosa, DL-8280 was 2 to 7 times more effective than norfloxacin and 7 to more than 50 times more active than pipemidic acid.
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PMID:In vitro and in vivo activity of DL-8280, a new oxazine derivative. 696 Aug 5

The incidence and antimicrobial susceptibility of organisms isolated from blood, urine and respiratory specimens at a teaching hospital in Hong Kong were studied retrospectively from 1986-1993. The incidence of Gram-positive bacteraemia, particularly coagulase-negative staphylococci (CNS), increased significantly from 33.6 to 47.3% (P < 0.001) while that of Gram-negative bacteraemia fell from 60.0 to 47.0% (P < 0.001). Among blood isolates, methicillin resistance of CNS increased from 17.0 to 58.0% (P < 0.001) and cefuroxime resistance of Enterobacter spp. increased from 21.0 to over 50% (P < 0.01). Among urinary isolates, cefuroxime resistance of Klebsiella spp. (11.0 to 24.0%, P < 0.001) and Enterobacter spp. (32.0 to 75.0%, P < 0.001) increased. Nalidixic acid resistance among Gram-negative urinary isolates, except Proteus mirabilis, rose by three- to sixfold. For Streptococcus pneumoniae, isolated from the respiratory tract, penicillin resistance increased dramatically (2 to 18%, P < 0.001). For respiratory isolates of Haemophilus influenzae, ampicillin resistance increased from 17.0 to 29.0% (P < 0.001). These data are useful in guiding empirical treatment of nosocomial infections.
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PMID:Changing patterns of susceptibilities of blood, urinary and respiratory pathogens in Hong Kong. 892 80

The detection of clinical isolates with decreased fluoroquinolone susceptibilities and a resistance mechanism is of epidemiological and clinical interest. We studied the susceptibilities of 62 clinical isolates and 2 American Type Culture Collection reference strains of Haemophilus influenzae to ciprofloxacin, levofloxacin, moxifloxacin, and nalidixic acid by the microdilution and disk diffusion methods. The ciprofloxacin MICs for 34 of the isolates were >/=0.12 micro g/ml (range, 0.12 to 32 micro g/ml), and the ciprofloxacin MICs for 28 matched control isolates were </=0.06 micro g/ml. In addition, we sequenced the quinolone resistance-determining regions (QRDRs) of gyrA and parC of all strains. The log(2) MICs of all quinolones were plotted against the inhibition zone diameters. The MICs and inhibition zone diameters selected to screen for the resistance mechanism were based on the susceptibility distribution data and the presence or absence of amino acid changes in the QRDRs of GyrA and ParC. Strains for which ciprofloxacin MICs were </=0.06 micro g/ml, levofloxacin and moxifloxacin MICs were </=0.03 micro g/ml, and nalidixic acid MICs were </=2.0 micro g/ml lacked modifications in the QRDR of GyrA. In contrast, all strains for which ciprofloxacin, levofloxacin, and moxifloxacin MICs were >/=0.5 micro g/ml and the vast majority of those for which nalidixic acid MICs were >/=32 micro g/ml exhibited amino acid changes in GyrA and ParC. Nalidixic acid and the other three fluoroquinolones studied could be used to screen H. influenzae isolates for the detection of decreased susceptibilities to quinolones due to the acquisition of two amino acid changes in the QRDRs of GyrA and ParC (sensitivity, >95%; specificity, >80%).
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PMID:Laboratory detection of Haemophilus influenzae with decreased susceptibility to nalidixic acid, ciprofloxacin, levofloxacin, and moxifloxacin due to GyrA and ParC mutations. 1500 73