Eperezolid

Modify Date: 2024-01-05 21:42:09

Eperezolid Structure
Eperezolid structure
Common Name Eperezolid
CAS Number 165800-04-4 Molecular Weight 394.39700
Density 1.37g/cm3 Boiling Point 701.2ºC at 760 mmHg
Molecular Formula C18H23FN4O5 Melting Point N/A
MSDS N/A Flash Point 377.9ºC

 Use of Eperezolid


Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).IC50 value: 1-4 mg/ml (MIC90, staphylococci) [1]Target: AntibioticEperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase [2]. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit [3].

 Names

Name N-[[(5S)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
Synonym More Synonyms

 Eperezolid Biological Activity

Description Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).IC50 value: 1-4 mg/ml (MIC90, staphylococci) [1]Target: AntibioticEperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase [2]. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit [3].
Related Catalog
References

[1]. Rybak MJ, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus f

[2]. Lin AH, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother. 1997 Oct;41(10):2127-31.

[3]. Zhou CC, et al. 1H nuclear magnetic resonance study of oxazolidinone binding to bacterial ribosomes. Antimicrob Agents Chemother. 2002 Mar;46(3):625-9.

 Chemical & Physical Properties

Density 1.37g/cm3
Boiling Point 701.2ºC at 760 mmHg
Molecular Formula C18H23FN4O5
Molecular Weight 394.39700
Flash Point 377.9ºC
Exact Mass 394.16500
PSA 102.42000
LogP 0.38670
Vapour Pressure 1.22E-20mmHg at 25°C
Index of Refraction 1.579
Storage condition 2-8℃

 Safety Information

HS Code 2934999090

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Eperezolid