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Arzneimittel-Forschung 1984O-3-amino-3-deoxy-alpha-D-glucopyranosyl-(1----6)-O-[2,6-diamino-2,3,4,6 -tetradeoxy-alpha-D-erythro-hexopyrano-hexopyranosyl-(1----4 ) ]-2-deoxy-L- streptamine...
O-3-amino-3-deoxy-alpha-D-glucopyranosyl-(1----6)-O-[2,6-diamino-2,3,4,6 -tetradeoxy-alpha-D-erythro-hexopyrano-hexopyranosyl-(1----4 ) ]-2-deoxy-L- streptamine (dibekacin), like other known aminoglycoside antibiotics, possesses a dose-dependent neuromuscular blocking activity in vivo. d-Tubocurarine, at a dose which per se does not influence the contraction of gastrocnemius muscle elicited by sciatic nerve stimulation, significantly potentiates the neuromuscular blockade produced by dibekacin. Neostigmine methylsulfate is unable to reverse the neuromuscular blocking activity of dibekacin, whereas calcium chloride antagonizes the neuromuscular blockade produced by this antibiotic.
Topics: Animals; Calcium; Dibekacin; In Vitro Techniques; Kanamycin; Male; Neostigmine; Neuromuscular Junction; Rats; Rats, Inbred Strains; Sciatic Nerve; Tubocurarine
PubMed: 6543128
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Jan 1981Dibekacin, a new parenteral aminoglycoside, was compared with gentamicin in vitro against 221 clinical isolates. Tests for minimum inhibitory concentrations, performed... (Comparative Study)
Comparative Study
Dibekacin, a new parenteral aminoglycoside, was compared with gentamicin in vitro against 221 clinical isolates. Tests for minimum inhibitory concentrations, performed in agar, demonstrated that dibekacin was comparable to gentamicin against most isolates tested. Dibekacin was slightly more active than gentamicin against some isolates of Pseudomonas aeruginosa, but was significantly less active against strains of Serratia.
Topics: Anti-Bacterial Agents; Bacteria; Dibekacin; Gentamicins; Kanamycin; Microbial Sensitivity Tests; Pseudomonas aeruginosa; Serratia marcescens
PubMed: 6787978
DOI: 10.1128/AAC.19.1.190 -
General Pharmacology 19891. Dibekacin (0.3-3 mM) reduced indirectly elicited twitches in rat phrenic-hemidiaphragm. This effect was potentiated in low extracellular calcium media. 2. The...
1. Dibekacin (0.3-3 mM) reduced indirectly elicited twitches in rat phrenic-hemidiaphragm. This effect was potentiated in low extracellular calcium media. 2. The blockade induced by dibekacin (3 mM) could be reversed by calcium (2.5 mM), 3,4-diamino-pyridine (3,4-DAP, 10 microM) or guanidine (3 mM), whereas neostigmine (3 microM), eserine (25 microM) or tetraethylammonium (100 microM) were less potent. 3. Dibekacin (3 mM) blocked directly-elicited twitches. Low concentrations were unable to obtain any effect. 4. It is concluded that dibekacin exerts its blocking action by limiting the calcium entry at motor nerve terminals, but a postsynaptic effect is also present. 3,4-DAP, guanidine and calcium were the most potent drugs in reversing the blockade.
Topics: Animals; Calcium; Diaphragm; Dibekacin; In Vitro Techniques; Kanamycin; Male; Muscle Contraction; Neuromuscular Blocking Agents; Neuromuscular Junction; Phrenic Nerve; Rats; Rats, Inbred Strains; Respiratory Muscles
PubMed: 2753347
DOI: 10.1016/0306-3623(89)90204-8 -
Antimicrobial Agents and Chemotherapy Sep 2015Corynebacterium striatum BM4687 was resistant to gentamicin and tobramycin but susceptible to kanamycin A and amikacin, a phenotype distinct among Gram-positive...
Corynebacterium striatum BM4687 was resistant to gentamicin and tobramycin but susceptible to kanamycin A and amikacin, a phenotype distinct among Gram-positive bacteria. Analysis of the entire genome of this strain did not detect any genes for known aminoglycoside resistance enzymes. Yet, annotation of the coding sequences identified 12 putative acetyltransferases or GCN5-related N-acetyltransferases. A total of 11 of these coding sequences were also present in the genomes of other Corynebacterium spp. The 12th coding sequence had 55 to 60% amino acid identity with acetyltransferases in Actinomycetales. The gene was cloned in Escherichia coli, where it conferred resistance to aminoglycosides by acetylation. The protein was purified to homogeneity, and its steady-state kinetic parameters were determined for dibekacin and kanamycin B. The product of the turnover of dibekacin was purified, and its structure was elucidated by high-field nuclear magnetic resonance (NMR), indicating transfer of the acetyl group to the amine at the C-3 position. Due to the unique profile of the reaction, it was designated aminoglycoside 3-N-acetyltransferase type XI.
Topics: Acetyltransferases; Anti-Bacterial Agents; Corynebacterium; Dibekacin; Kanamycin; Microbial Sensitivity Tests; Molecular Structure
PubMed: 26149994
DOI: 10.1128/AAC.01203-15 -
Carbohydrate Research Oct 19966-O-(3-Oxa-2,3,4-trideoxy-alpha-D-glycero-hexopyranosyl) derivatives (10 and 17) of both 3',4'-dideoxyneamine and 5-epifluoro-5,3',4'-trideoxyneamine have been prepared...
6-O-(3-Oxa-2,3,4-trideoxy-alpha-D-glycero-hexopyranosyl) derivatives (10 and 17) of both 3',4'-dideoxyneamine and 5-epifluoro-5,3',4'-trideoxyneamine have been prepared by coupling ethyl 6-O-benzyl-3-oxa-2,3,4-trideoxy-1-thio-D-glycero-hexopyranoside (5) with suitable aglycons. The corresponding 3"-aza derivative (19) of dibekacin (6) was prepared by oxidation of 1,3,2',6'-tetra-N-tosyldibekacin (7) with Pb(OAc)4 followed by treatment with NH4OAc and reduction with NaBH3CN. Related ring-opening compounds (11 and 25) were also prepared.
Topics: Anti-Bacterial Agents; Carbohydrate Sequence; Dibekacin; Glycosides; Magnetic Resonance Spectroscopy; Molecular Sequence Data; Molecular Structure; Oligosaccharides
PubMed: 8916543
DOI: 10.1016/0008-6215(96)00176-0 -
Comptes Rendus Des Seances de... 1983We compare the acute toxicity of a dose of gentamicin or dibekacin in Mice at different times of the day. The female Mice are housed with food and water ad libitum for... (Comparative Study)
Comparative Study
We compare the acute toxicity of a dose of gentamicin or dibekacin in Mice at different times of the day. The female Mice are housed with food and water ad libitum for one and half week, ten or fifteen per cage in a light controlled room (lights on from 8 to 20 hrs). Each animal was given gentamycin (250, 275, 300 or 325 mg/kg) intramuscular and dibekacin (320, 355, 390, 425 or 460 mg/kg) at one of four times: 8, 14, 20 and 2 hrs). After injection, the animals are kept in their cages and observed for 10 days. We show that the circadian biosusceptibility rhythm in dibekacin toxicity is similar to that of gentamycin with significant differences in the mortality at the four hours. There is an evident parallelism between the curves for gentamycin and dibekacin but the differences in the percentage of mortality rate are more important for gentamycin than for dibekacin.
Topics: Animals; Circadian Rhythm; Dibekacin; Female; Gentamicins; Kanamycin; Mice
PubMed: 6421462
DOI: No ID Found -
The Journal of Antimicrobial... Nov 1980
Topics: Adult; Aged; Aging; Dibekacin; Female; Humans; Kanamycin; Kinetics; Male
PubMed: 7440467
DOI: 10.1093/jac/6.6.737 -
Annales de L'Institut Pasteur.... 1985Radioimmunoassay, rate nephelometric inhibition immunoassay and substrate-labelled fluorescent immunoassay were employed for the quantitative determination of dibekacin...
Radioimmunoassay, rate nephelometric inhibition immunoassay and substrate-labelled fluorescent immunoassay were employed for the quantitative determination of dibekacin in serum. The cross-reactivity of the antibody provided with each assay allowed the use of tobramycin assay procedures for measuring dibekacin concentrations. With radioimmunoassay and nephelometric immunoassay, a dibekacin calibration curve was required, whereas fluorescent immunoassay was directly suitable for dibekacin assay, with cross-reactivity of nearly 100%. This allows the purchase of one assay kit for testing two antibiotics and thus reduces the cost to medical laboratories.
Topics: Cross Reactions; Dibekacin; Fluorescent Antibody Technique; Humans; Kanamycin; Nephelometry and Turbidimetry; Radioimmunoassay; Reagent Kits, Diagnostic; Tobramycin
PubMed: 3901881
DOI: 10.1016/s0769-2609(85)80100-9 -
The Tohoku Journal of Experimental... Sep 1986Electron microscopy of thin sections of Pseudomonas aeruginosa IAM 1007 treated with dibekacin revealed blebs, disintegration of the outer membrane of the cell wall and...
Electron microscopy of thin sections of Pseudomonas aeruginosa IAM 1007 treated with dibekacin revealed blebs, disintegration of the outer membrane of the cell wall and degenerative features of the cytoplasm. In the next experiment, the cell wall fraction was isolated from the mechanically disrupted cells, incubated with dibekacin and was subjected to electron microscopy, in order to find a clue to the action mechanism of dibekacin on the cell wall of Pseudomonas aeruginosa IAM 1007. As a result, it was found that unidentified substances were released from the surface of the cell wall and that the outer membrane of the cell wall disappeared. The degree of changes of the cell wall ultrastructure was almost proportional to the length of incubation with dibekacin. These findings strongly suggest that dibekacin directly disintegrates the outer membrane of the cell wall of Pseudomonas aeruginosa IAM 1007.
Topics: Cell Membrane; Cell Nucleus; Cell Wall; Cytoplasm; Dibekacin; Kanamycin; Microscopy, Electron; Pseudomonas aeruginosa
PubMed: 3095954
DOI: 10.1620/tjem.150.69 -
Journal of Clinical Microbiology Jan 201616S rRNA methyltransferases confer resistance to most aminoglycosides, but discriminating their activity from that of aminoglycoside-modifying enzymes (AMEs) is...
16S rRNA methyltransferases confer resistance to most aminoglycosides, but discriminating their activity from that of aminoglycoside-modifying enzymes (AMEs) is challenging using phenotypic methods. We demonstrate that arbekacin, an aminoglycoside refractory to most AMEs, can rapidly detect 16S methyltransferase activity in Enterobacteriaceae with high specificity using the standard disk susceptibility test.
Topics: Anti-Infective Agents; Dibekacin; Disk Diffusion Antimicrobial Tests; Drug Resistance, Bacterial; Enterobacteriaceae; Genotype; Humans; Phenotype; RNA, Ribosomal, 16S; tRNA Methyltransferases
PubMed: 26537447
DOI: 10.1128/JCM.02642-15