novobiocin and Bacterial-Infections

Topics: Adenosine Triphosphate; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Bacterial Proteins; Drug Design; Humans; Models, Molecular; Molecular Targeted Therapy

Topics: Ampicillin; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Cell Wall; Cephalosporins; Chloramphenicol; Drug Combinations; Enterobacter; Erythromycin; Escherichia coli; Gentamicins; Humans; Kanamycin; Klebsiella; Lincomycin; Neomycin; Novobiocin; Penicillin Resistance; Penicillins; Polymyxins; Proteus; Pseudomonas aeruginosa; Streptomycin; Tetracycline

Topics: Animals; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Chemical Phenomena; Chemistry; Coumarins; Disease Models, Animal; Dogs; Drug Resistance, Microbial; Humans; Mice; Novobiocin; Rats; Species Specificity; Streptomyces; Structure-Activity Relationship

The aim of this study was to determine the efficacy of novobiocin and rifampin as oral antibiotic prophylaxis for the prevention of catheter-related infection in melanoma patients treated with interleukin-2 (IL-2) plus interferon-alpha and chemotherapy (biochemotherapy).. Patients with advanced melanoma who were treated with biochemotherapy at the University of Texas M. D. Anderson Cancer Center were randomized in a crossover study to receive either oral antibiotic prophylaxis consisting of novobiocin and rifampin or observation alone over a 35-day course period. Patients were subsequently "crossed over" to the opposite arm of the study for an additional 35-day period, with each serving as his or her own control.. Twenty-six patients were enrolled. Nine patients (35%) failed to tolerate oral antibiotics because of severe nausea and vomiting; 17 patients (65%) were crossed over and considered evaluable. During the control patient courses, 71% of evaluable patients had infectious complications, 41% had a catheter-associated bacteremia, and 53% had a local catheter infection. In contrast, of the patients treated with antibiotic prophylaxis, only 12% had an infectious complication (P = 0.001), 12% had a local catheter infection (P = 0.008), and 6% had catheter-associated bacteremias (P = 0.04). Thirty-six episodes of catheter infections occurred during the 17 control courses, whereas only 3 episodes occurred during antibiotic prophylaxis (P < 0.001).. Although more than one-third of patients receiving IL-2 treatment with biochemotherapy failed to tolerate novobiocin and rifampin, this oral antibiotic regimen was efficacious in preventing the infectious complications, especially those associated with vascular catheters, in this high risk patient population.

Topics: Administration, Oral; Adult; Anti-Bacterial Agents; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Bacteremia; Bacterial Infections; Catheterization, Central Venous; Catheterization, Peripheral; Catheters, Indwelling; Chemoprevention; Cross-Over Studies; Equipment Contamination; Female; Humans; Immunologic Factors; Interferon-gamma; Interleukin-2; Male; Melanoma; Middle Aged; Nausea; Novobiocin; Prospective Studies; Rifampin; Vomiting

Topics: Adolescent; Adult; Aged; Bacterial Infections; Child; Clinical Trials as Topic; Drug Combinations; Humans; Middle Aged; Novobiocin; Tetracycline; Time Factors

Metal complexes of Schiff bases derived from sulfamethoxazole (SMZ) and sulfathiazole (STZ), converted to their β-lactam derivatives have been synthesized and experimentally characterized by elemental analysis, spectral (IR, (1)H NMR, (13)C NMR, and EI-mass), molar conductance measurements and thermal analysis techniques. The structural and electronic properties of the studied molecules were investigated theoretically by performing density functional theory (DFT) to access reliable results to the experimental values. The spectral and thermal analysis reveals that the Schiff bases act as bidentate ligands via the coordination of azomethine nitrogen to metal ions as well as the proton displacement from the phenolic group through the metal ions; therefore, Cu complexes can attain the square planner arrangement and Zn complexes have a distorted tetrahedral structure. The thermogravimetric (TG/DTG) analyses confirm high stability for all complexes followed by thermal decomposition in different steps. In addition, the antibacterial activities of synthesized compounds have been screened in vitro against various pathogenic bacterial species. Inspection of the results revealed that all newly synthesized complexes individually exhibit varying degrees of inhibitory effects on the growth of the tested bacterial species, therefore, they may be considered as drug candidates for bacterial pathogens. The free Schiff base ligands (1-2) exhibited a broad spectrum antibacterial activity against Gram negative Escherichia coli, Pseudomonas aeruginosa, and Proteus spp., and Gram positive Staphylococcus aureus bacterial strains. The results also indicated that the β-lactam derivatives (3-4) have high antibacterial activities on Gram positive bacteria as well as the metal complexes (5-8), particularly Zn complexes, have a significant activity against all Gram negative bacterial strains. It has been shown that the metal complexes have significantly higher activity than corresponding ligands due to chelation process which reduces the polarity of metal ion by coordinating with ligands.

Topics: Anti-Bacterial Agents; Azoles; Bacteria; Bacterial Infections; beta-Lactams; Coordination Complexes; Humans; Ligands; Microbial Sensitivity Tests; Models, Molecular; Schiff Bases; Sulfamethoxazole; Sulfathiazole; Sulfathiazoles

QPT-1 was discovered in a compound library by high-throughput screening and triage for substances with whole-cell antibacterial activity. This totally synthetic compound is an unusual barbituric acid derivative whose activity resides in the (-)-enantiomer. QPT-1 had activity against a broad spectrum of pathogenic, antibiotic-resistant bacteria, was nontoxic to eukaryotic cells, and showed oral efficacy in a murine infection model, all before any medicinal chemistry optimization. Biochemical and genetic characterization showed that the QPT-1 targets the beta subunit of bacterial type II topoisomerases via a mechanism of inhibition distinct from the mechanisms of fluoroquinolones and novobiocin. Given these attributes, this compound represents a promising new class of antibacterial agents. The success of this reverse genomics effort demonstrates the utility of exploring strategies that are alternatives to target-based screens in antibacterial drug discovery.

Topics: Animals; Anti-Bacterial Agents; Area Under Curve; Bacteria; Bacterial Infections; Bacterial Proteins; Cell Line; Cell Proliferation; Metabolic Clearance Rate; Mice; Microbial Sensitivity Tests; Molecular Structure; Staphylococcus aureus; Stereoisomerism; Topoisomerase II Inhibitors

A study was conducted to determine whether intramammary antibiotic treatment of heifer mammary glands following the first milking after calving was effective for reducing the percentage of mammary quarters infected during early lactation. Jersey and Holstein heifers from two research herds were assigned to one of three treatment groups: (1) no intramammary infusion following the first milking after parturition, (2) intramammary infusion of all quarters with pirlimycin hydrochloride following the first milking after parturition and (3) intramammary infusion of all quarters with novobiocin sodium plus penicillin G procaine following the first milking after parturition. Almost 93% of Jersey heifers (40/43) and 73.1% of quarters (125/171) were infected at the first milking. Almost 77% of quarters (33/43) were cured following treatment with pirlimycin, 61.8% (21/34) were cured following treatment with penicillin-novobiocin and 39.6% (19/48) of infections were eliminated spontaneously in the untreated control group. Significantly fewer infections were observed in pirlimycin or penicillin-novobiocin treated mammary glands of Jersey heifers during early lactation than in untreated control mammary glands. Almost 89% of Holstein heifers (32/36) and 52.8% of quarters (76/144) were infected at the first milking. About 57% (12/21) of quarters were cured following treatment with pirlimycin, 41.4% (12/29) were cured following treatment with penicillin-novobiocin and 23.1% (6/26) of infections were eliminated spontaneously in the untreated negative control group. Significantly fewer infections were observed in pirlimycin treated mammary glands of Holstein heifers during early lactation than in untreated control mammary glands. However, no significant differences were observed following penicillin-novobiocin treatment of Holstein heifers after the first milking of lactation compared with untreated control quarters. Coagulase-negative staphylococci, Streptococcus uberis and Streptococcus dysgalactiae subsp dysgalactiae were isolated most frequently in heifers from both herds.

Topics: Animals; Anti-Bacterial Agents; Bacterial Infections; Cattle; Cattle Diseases; Clindamycin; Female; Infusions, Parenteral; Mammary Glands, Animal; Milk; Novobiocin; Parturition; Penicillins; Pregnancy

Topics: Animals; Anti-Bacterial Agents; Bacterial Infections; Cephalosporins; Dose-Response Relationship, Drug; Humans; Novobiocin; Penicillin G; Penicillin V

Topics: Animals; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Chloramphenicol; Chlortetracycline; Dihydrostreptomycin Sulfate; Drug Stability; Erythromycin; Gastric Juice; Hydrogen-Ion Concentration; Kanamycin; Male; Mice; Microbial Sensitivity Tests; Novobiocin; Penicillin Resistance; Penicillins; Pneumococcal Infections; Rifampin; Solutions; Staphylococcal Infections; Staphylococcus; Streptococcal Infections

Topics: Bacterial Infections; Bilirubin; Candidiasis; Child, Preschool; Drug Eruptions; Female; Humans; Hyperbilirubinemia; Infant; Infant, Newborn; Infant, Newborn, Diseases; Infant, Premature; Infant, Premature, Diseases; Male; Novobiocin; Prognosis; Time Factors

Topics: Anti-Bacterial Agents; Bacitracin; Bacterial Infections; Cataract; Cataract Extraction; Cephalothin; Chloramphenicol; Colistin; Drug Therapy; Erythromycin; Eye Diseases; Humans; Kanamycin; Neomycin; Novobiocin; Penicillins; Polymyxins; Postoperative Complications; Sulfadiazine; Tetracycline; Toxicology; Vancomycin