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Chemical Compound Review:

YM-044 sodium(5R,6S)-6-(1- hydroxyethyl)-7-oxo-3...

Synonyms:

Rylander, M. et al., Bergan, T. et al., DeGuchi, Y. et al., Inoue, E. et al., Nord, C.E. et al.

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Disease relevance of (5R,6S)-6-(1-hydroxyethyl)-7-oxo-3-[(2R)-oxolan-2-yl]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid

Susceptibility of anaerobic bacteria to ALP 201 [1].
Against Providencia spp., Proteus spp., and Haemophilus influenzae, SY5555 was less active than cefixime or cefteram [2].
Pseudomonas aeruginosa and Clostridium difficile were resistant to ALP-201 [3].
The minimum inhibitory concentration (MIC) of the new penem ALP 201 was tested against 243 recent clinical isolates of which 95 were from the family Enterobacteriaceae, 50 were from the genus Streptococcus, 50 were Staphylococcus aureus and 48 were Staphylococcus epidermidis [4].
ALP-201 was found to be highly active against Escherichia coli, Klebsiella spp., Enterobacter spp., Haemophilus influenzae, Branhamella catarrhalis, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, anaerobic cocci, Propioni-bacterium acnes, Clostridium perfringens, Bacteroides fragilis, Bacteroides spp. and fusobacteria [3].

High impact information on (5R,6S)-6-(1-hydroxyethyl)-7-oxo-3-[(2R)-oxolan-2-yl]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid

In vitro antibacterial activity and beta-lactamase stability of SY5555, a new oral penem antibiotic [2].
Further investigations are warranted with ALP-201, which is absorbed from the gastrointestinal tract after oral administration [3].
Furthermore, good coincidences were obtained between the unbound concentrations of SY5555 in lung and muscle interstitial fluids estimated from the total concentrations in homogenized tissues and those extrapolated by the microdialysis studies [5].

Analytical, diagnostic and therapeutic context of (5R,6S)-6-(1-hydroxyethyl)-7-oxo-3-[(2R)-oxolan-2-yl]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid

When tested against aerobic bacteria using a high inoculum or using the broth dilution technique, the activity of ALP-201 showed little dependence on inoculum size and the bactericidal activity was similar to the inhibitory activity [3].

References

Susceptibility of anaerobic bacteria to ALP 201. Nord, C.E., Lindmark, A., Persson, I. Antimicrob. Agents Chemother. (1989) [Pubmed]
In vitro antibacterial activity and beta-lactamase stability of SY5555, a new oral penem antibiotic. Inoue, E., Mitsuhashi, S. Antimicrob. Agents Chemother. (1994) [Pubmed]
Comparative in vitro activity of the new oral penem ALP-201 against aerobic and anaerobic bacteria. Rylander, M., Nord, C.E., Norrby, S.R. Eur. J. Clin. Microbiol. Infect. Dis. (1989) [Pubmed]
Comparative antibacterial activity of the penem ALP 201. Bergan, T., da Fonseca, J. Chemotherapy. (1991) [Pubmed]
An application of microdialysis to drug tissue distribution study: in vivo evidence for free-ligand hypothesis and tissue binding of beta-lactam antibiotics in interstitial fluids. DeGuchi, Y., Terasaki, T., Yamada, H., Tsuji, A. J. Pharmacobio-dyn. (1992) [Pubmed]

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