Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0519030 (Klebsiella)
 21,988 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The in vitro effects of the single agents, and the synergistic/antagonistic action of three different combinations of ampicillin (AMP, CAS 69-53-4), cefotaxime (CTX, CAS 63527-52-6), mezlocillin (MEZ, CAS 51481-65-3), and piperacillin (PIP, CAS 61477-96-1) with the beta-lactamase inhibitor sulbactam (SUL, CAS 68373-14-8) were determined against 675 gram-positive and gram-negative, both aerobic and anaerobic bacteria. All the combinations of sulbactam and the antibiotics (1: 1, 1:2 and 1:4) exhibited very similar synergistic action. The percentage of the total strains tested for which synergistic activity was found was 51% with SUL + AMP (1:1), 24% with SUL + CTX (1:1), 31% with SUL + MEZ (1:1), and 28% with SUL + PIP (1:1). A fourfold or greater reduction of MIC's in the comparison with the antibiotics alone was found with 23% of the total strains tested for the SUL + AMP, with 9% of the strains tested with SUL + CTX, with 11% of the strains tested with SUL + MEZ, and with 15% of the strains tested with the SUL + PIP-combination. In the presence of sulbactam, 18% of the strains tested showed a significant reduction in the number of resistant strains with ampicillin, 7% with cefotaxime, 16% with mezlocillin, 14% with piperacillin, and in parallel there was an increase in the number of fully susceptible strains (shift from resistant or moderately sensitive to sensitive) by about 14%. In comparison with the antibiotic alone, the most marked reductions in the number of resistant strains on combination with sulbactam were as follows (the percentage of reduction is shown in brackets): for SUL + AMP and Acine-tobacter spp. (39% fewer resistant strains). Citrobacter spp. (-60%), Enterobacter aerogenes (-48%), Klebsiella oxytoca (-49%), Klebsiella pneumoniae (-63%), Morganella morganii (-74%), and Proteus vulgaris (-55%); for SUL + CTX and Acinetobacter spp. (-38%), Enterobacter cloacae (-6%), Klebsiella pneumoniae (-16%), Serratia marcescens (-9%), and Bacteroides fragilis (-31%); for SUL + MEZ and Acinetobacter spp. (-68%), Citrobacter spp. (-27%), Enterobacter spp. (-23%), Klebsiella pneumoniae (-32%), and Serratia marcescens (-19%); for SUL + PIP and Acinetobacter spp. (-41%), Citrobacter spp. (-30%), Klebsiella spp. (-30%), and Serratia marcescens (-33%).
 ...
PMID:In vitro activity against clinically important gram-positive and gram-negative bacteria of sulbactam, alone and in combination with ampicillin, cefotaxime, mezlocillin, and piperacillin. 229 54

The ability of 22 strains of intestinal bacteria to bind the mutagenic pyrolyzates--3-amino-1,4-dimethyl-5H-pyrido-[4,3-b]indole [(Trp-P-1) CAS: 62450-06-0], 3-amino-1-methyl-5H-pyrido [4,3-b]indole [(Trp-P-2) CAS: 62450-07-1], 2-amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole [(Glu-P-1) CAS: 67730-11-4], 2-aminodipyrido[1,2-a:3',2'-d]imidazole [(Glu-P-2) CAS: 67730-10-3], 2-amino-3-methylimidazo[4,5-f]quinoline [(IQ) CAS: 76180-96-6], 2-amino-3,4-dimethylimidazo[4,5-f]quinoline [(MeIQ) CAS: 77094-11-2], and 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline [(MeIQx) CAS: 77500-04-0]--was investigated and compared to their ability to bind to some dietary fibers (corn bran, apple pulp, soy bean fiber, cellulose, chitin, and chitosan). The pyrolyzates are potent mutagenic and carcinogenic heterocyclic amines formed during cooking. Solution of these amines was mixed with aqueous suspension of bacterial cells or dietary fibers, and removal of these amines from the reaction mixture by centrifugation was defined as the binding. Trp-P-1 and Trp-P-2 were effectively bound to all gram-positive and some gram-negative bacterial cells, corn bran, apple pulp, and soy bean fiber. Binding of Trp-P-1 and Trp-P-2 to Escherichia coli, Klebsiella pneumoniae, and cellulose was moderate, and to chitin and chitosan it was little. None but corn bran bound Glu-P-1 and Glu-P-2 effectively. Corn bran effectively bound all mutagens tested. The quantity of the binding of IQ, MeIQ, and MeIQx was dependent on the strain of bacteria and the kind of fiber. The mechanism of binding of Trp-P-2 to freeze-dried feces, Lactobacillus casei YIT 9018 (LC9018), and corn bran was investigated. The binding was pH dependent, occurred instantaneously, and was inhibited by the addition of metal salts. These results indicate that the binding was mostly due to a cation-exchange mechanism, but some irreversible binding of Trp-P-2 was observed, most notably to freeze-dried feces. The mutagenicity of Trp-P-2 for Salmonella typhimurium TA98 in the presence of S9 mix was inhibited by the addition of LC9018 or corn bran to the reaction mixture. The results indicate that bound Trp-P-2 did not cause mutation under the assay conditions.
 ...
PMID:In vitro binding of potent mutagenic pyrolysates to intestinal bacteria. 301 97

Cefodizime (CAS 69739-16-8, HR 221) is a new third-generation cephalosporin with pharmacokinetic properties that make it suitable for once-daily administration in the treatment of lower respiratory tract infections (LRTI). Ninety-nine adult hospitalized patients (66 males, 33 females, median age 57.5 years) received a once-daily injection of 2 g cefodizime for LRTI. Median treatment duration was 8 days. Forty-two patients received cefodizime intravenously and 57 intramuscularly. Indications for treatment were as follows; primary lobar pneumonia (n = 36), bronchopneumonia (n = 14), secondary pneumonia (n = 3), aspiration pneumonia (n = 5), acute exacerbation of chronic bronchitis (n = 21), and of bronchiectasis (n = 9) and acute purulent bronchitis (n = 11). General condition was good in 29 patients and poor in 58; 12 patients were critically ill. The following pathogens were isolated at baseline (source: bronchial secretions, sputum or blood): S. pneumoniae (n = 47), Haemophilus spp. (n = 17), M. catarrhalis (n = 6), Streptococcus spp. (n = 9), Staphylococcus spp. (n = 5), Klebsiella spp. (n = 4), Pseudomonas spp. (n = 1), A. calcoaceticus (n = 1) and anaerobic organisms (n = 7). Fifty-nine patients were evaluable for bacteriological response and 82 for clinical response. Bacteriological outcome was satisfactory in 29/30 patients having LRTI with parenchymal involvement (97%) and in 29/29 patients without parenchymal involvement (100%). Clinical cure was achieved in 41/43 evaluable patients with parenchymal involvement (95%) and in 37/39 patients without parenchymal involvement (95%) in the per-protocol analysis and in 54/58 patients (93%) and 37/41 patients (93%), respectively, in the clinical intention-to-treat analysis. Three of the patients with an unsatisfactory clinical response died of infection during the study. Cefodizime was well tolerated. Adverse reactions--all of mild intensity--were tachycardia, lumbalgia and dizziness, each occurring in one patient. Cefodizime 2 g once daily either i.m. or i.v. was effective in the treatment of lower respiratory tract infections in hospitalized patients.
 ...
PMID:Cefodizime once daily in the treatment of lower respiratory tract infections. 920 86

Serum sensitivity and surface hydrophobicity of two Klebsiella pneumoniae strains (internal strain No. 378 and 3259) exposed to imipenem (CAS 64221-86-9) and meropenem (CAS 96036-03-2) at subinhibitory concentrations (sub-MICs; 1/4, 1/8 and 1/16 of the MICs) were evaluated. Carbapenems at all sub-MICs tested (with the exception of 1/16 of the MICs in strain 378) decreased susceptibility of bacteria to serum bactericidal activity. All sub-MICs of the antibiotics tested also reduced the bacterial surface hydrophobicity. The surface hydrophobicity of strain 3259 was most effectively decreased after the exposure to imipenem and meropenem at 1/4 of the MICs (to 3% or 5.2% of the control values). The highest decrease of hydrophobicity in strain 378 was found after exposure to imipenem and meropenem at 1/16 of the MICs (19.2% or 32.3%).
 ...
PMID:Effects of imipenem and meropenem on serum sensitivity and surface hydrophobicity of Klebsiella pneumoniae. 985 Apr 33

Thiamphenicol-glycinate-acetylcysteinate (TGA; CAS 20192-91-0) is widely used for the treatment of infections of varied aetiology. The aim of this study was to compare the antibacterial activity of thiamphenicol-glycinate (TG; CAS 15318-45-3), TGA, amoxicillin (CAS 61336-70-7) plus clavulanic acid (CAS 58001-44-8), azithromycin (CAS 83905-01-5) and ceftriaxone (CAS 104376-79-6). Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined against Staphylococcus aureus, Klebsiella pneumoniae, Streptococcus pyogenes, Streptococcus pneumoniae, Moraxella catarrhalis and Haemophilus influenzae according to the National Committee for Clinical Laboratory Standards (NCCLS) methods. The effects of changes in assay conditions were also examined. The activity of TG and TGA was similar to that of amoxicillin plus clavulanic acid, with the exception of methicillin resistant S. aureus. Azithromycin and ceftriaxone were characterised by a limited activity against gram-positive cocci and methicillin resistant and cefinase-positive S. aureus, respectively. TG and TGA are characterized by a wide spectrum of activity, comparable to that of recent commercialized antibiotics for treatment of respiratory tract infections.
 ...
PMID:Comparative in vitro activity of thiamphenicol-glycinate and thiamphenicol-glycinate-acetylcysteinate and other antimicrobials against respiratory pathogens. 1136 73

Moxifloxacin (CAS 186286-86-8) is a recent fluoroquinolone addressed to the treatment of respiratory infections, although clinical efficacy has been shown also in the therapy of urinary tract diseases. The in vitro activity of moxifloxacin against one encapsulated strain of Klebsiella pneumoniae was determined by means of time-kill curves and by evaluation of effects of subinhibitory concentrations on bacterial morphology by means of scanning electron microscopy. Moreover, the efficacy and time requested to eradicate the same strain from lungs was determined after intratracheal infection of guinea pigs. K. pneumoniae was rapidly killed by moxifloxacin at concentrations greater than the minimum inhibitory concentration (MIC). Subinhibitory concentrations (1/4 and 1/8 of the MIC ) induced filamentation in a remarkable portion of bacteria. A progressive decrease in the bacterial content of lungs was observed during the 48-h period, with statistically significant differences compared with the control animals. In conclusion, this study provides in vivo evidence of the antimicrobial properties of moxifloxacin against K. pneumoniae.
 ...
PMID:Evaluation of antibacterial in vitro activity of moxifloxacin and its effects on pulmonary clearance of Klebsiella pneumoniae in an animal experimental model. 1614 16

In the present study, 20 new compounds having 3-[2-(5-aryl-1,3,4-oxadiazol-2-yl) imino-4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-indole-2-one (I-XII) and 3-[2-(4-carbethoxymethylthiazol-2-yl)imino-4-thiazoldinon-5-ylidenel-5-substituted/nonsubstituted IH-indole-2-one (XIII-XX) systems were synthesized. The structures were confirmed by spectral methods (UV, IR, 1H-NMR, 13C-NMR, 13C-DEPT (135), electron impact mass spectrometry) and elemental analysis. All compounds were tested for in vitro antimicrobial activity against Staphylococcus aureus ATCC 6538, Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 8739, Klebsiella pneumoniae ATCC 4352, Pseudomonas aeruginosa ATCC 1539, Salmonella typhi, Shigella flexneri, Proteus mirabilis ATCC 14153, Candida albicans ATCC 10231, Microsporum gypseum (NCPF-580), Microsporum canis, Trichophyton mentagrophytes and Trichophyton rubrum and some of them were found to be active. Especially, compound I was more active than cefuroxime sodium (CAS 56238-63-2) which was used as a standard, and the activity of compound XII was close to that of cefuroxime sodium against Staphylococcus epidermidis ATCC 12228. Primary screening for antituberculous activity was conducted at 6.25 microg/ml against Mycobacterium tuberculosis H37Rv in BACTEC 12B medium using the BACTEC 460 radiometric system. The anticonvulsant activities of selected prototoype compounds (I, IV-VI, VIII, XI, XIII, XVI-XVIII) administered at doses of 50-200 mg/kg (i.p.) were evaluated using the pentetrazol test (PTZ) in mice.
 ...
PMID:Synthesis and evaluation of antimicrobial and anticonvulsant activities of some new 3-[2- (5-aryl-1,3,4-oxadiazol-2-yl/4-carbethoxymethylthiazol-2-yl) imino-4-thiazolidinon-5-ylidene]-5-substituted/nonsubstituted 1H-indole-2-ones and investigation of their structure-activity relationships. 1661 17

Although citrulline malate (CM; CAS 54940-97-5, Stimol) is used against fatigue states, its anti-asthenic effect remains poorly documented. The objective of this double-blind study was to evaluate the effect of oral ingestion of CM on a rat model of asthenia, using in situ (31)Phosphorus magnetic resonance spectroscopy ((31)P-MRS). Muscle weakness was induced by intraperitoneal injections of Klebsiella pneumoniae endotoxin (lipopolysaccharides at 3 mg/kg) at t(0) and t(0)+24 h. For each animal, muscle function was investigated strictly non-invasively before (t(0)-24 h) and during (t(0)+48 h) endotoxemia, through a standardized rest-stimulation-recovery protocol. The transcutaneous electrical stimulation protocol consisted of 5.7 min of repeated isometric contractions at a frequency of 3.3 Hz, and force production was measured with an ergometer. CM supplementation in endotoxemic animals prevented the basal phosphocreatine/ATP ratio reduction and normalized the intracellular pH (pH(i)) time-course during muscular activity as a sign of an effect at the muscle energetics level. In addition, CM treatment avoided the endotoxemia-induced decline in developed force. These results demonstrate the efficiency of CM for limiting skeletal muscle dysfunction in rats treated with bacterial endotoxin.
 ...
PMID:Beneficial effects of citrulline malate on skeletal muscle function in endotoxemic rat. 1903 44