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Chemical Compound Review

Doyle     (2R,5R,6S)-6-[[(2R)-2-[[(2R)- 2-amino-3...

Synonyms: ASPC, Aspoxicilina, Aspoxicillan, aspoxicillin, Aspoxicilline, ...
 
 
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Disease relevance of Aspoxicillan

 

High impact information on Aspoxicillan

  • Our detailed analysis of the affinities of the PBPs of A. pleuropneumoniae and of the bacterial lysis kinetics for several beta-lactam antibiotics revealed that the strong antibacterial activity of aspoxicillin against this strain could be related to the higher affinity of PBP 3 and that preferential inactivation of PBP 1b could cause rapid lysis [5].
  • Growth suppression by sub-MICs of aspoxicillin was examined in vitro using either previously unexposed bacterial cells or cells which had been pre-exposed to twice the MIC of aspoxicillin for 2 h [1].
  • In acute toxicity, TA-058 showed good tolerance in mice (LD50 greater than 10 g/kg, i.v.) [4].
  • A new model of bacterial peritonitis in mice for evaluation of antibiotics. Effects of aspoxicillin and piperacillin [6].
  • Pharmacokinetics of aspoxicillin in subjects with normal and impaired renal function [7].
 

Anatomical context of Aspoxicillan

 

Analytical, diagnostic and therapeutic context of Aspoxicillan

  • The method enabled the determination of aspoxicillin at concentrations below 100 ng/ml, with a linear calibration curve at concentrations of 1-1000 ng/ml for 100 microliters of lavage fluid [8].
  • Determination of aspoxicillin in broncho-alveolar lavage fluid by high-performance liquid chromatography with photolysis and electrochemical detection [8].
  • Both the separation and determination of aspoxicillin in human plasma by micellar electrokinetic chromatography (MEKC) were investigated [9].

References

  1. Activity of sub-minimal inhibitory concentrations of aspoxicillin in prolonging the postantibiotic effect against Staphylococcus aureus. Oshida, T., Onta, T., Nakanishi, N., Matsushita, T., Yamaguchi, T. J. Antimicrob. Chemother. (1990) [Pubmed]
  2. An experimental meningitis with Streptococcus pneumoniae in rats: therapeutic effect of aspoxicillin and its penetration into CSF. Yamaguchi, T., Kasuga, O., Okuno, S., Maezawa, I. Drugs under experimental and clinical research. (1989) [Pubmed]
  3. Therapeutic effect of aspoxicillin on experimental pneumonia with Klebsiella pneumoniae in mice. Yamaguchi, T., Ishii, N., Tani, K., Matsushita, T., Matsumoto, K. Drugs under experimental and clinical research. (1989) [Pubmed]
  4. Synthesis and antibacterial activity of asparagine derivatives of aminobenzylpenicillin. Wagatsuma, M., Seto, M., Miyagishima, T., Kawazu, M., Yamaguchi, T., Ohshima, S. J. Antibiot. (1983) [Pubmed]
  5. Morphological changes and lysis induced by beta-lactams associated with the characteristic profiles of affinities of penicillin-binding proteins in actinobacillus pleuropneumoniae. Inui, T., Endo, T., Matsushita, T. Antimicrob. Agents Chemother. (2000) [Pubmed]
  6. A new model of bacterial peritonitis in mice for evaluation of antibiotics. Effects of aspoxicillin and piperacillin. Matsushita, T., Okuno, S., Maezawa, I., Ohshima, S., Yamaguchi, T., Sawada, Y., Hashimoto, I., Nakamura, T. The Japanese journal of antibiotics. (1989) [Pubmed]
  7. Pharmacokinetics of aspoxicillin in subjects with normal and impaired renal function. Geyer, J., Höffler, D., Koeppe, P. Arzneimittel-Forschung. (1988) [Pubmed]
  8. Determination of aspoxicillin in broncho-alveolar lavage fluid by high-performance liquid chromatography with photolysis and electrochemical detection. Yamazaki, T., Ishikawa, T., Nakai, H., Miyai, M., Tsubota, T., Asano, K. J. Chromatogr. (1993) [Pubmed]
  9. Separation and determination of aspoxicillin in human plasma by micellar electrokinetic chromatography with direct sample injection. Nishi, H., Fukuyama, T., Matsuo, M. J. Chromatogr. (1990) [Pubmed]
 
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