Radezolid

Modify Date: 2024-07-22 18:04:54

Radezolid Structure
Radezolid structure
Common Name Radezolid
CAS Number 869884-78-6 Molecular Weight 438.455
Density 1.3±0.1 g/cm3 Boiling Point 712.5±60.0 °C at 760 mmHg
Molecular Formula C22H23FN6O3 Melting Point N/A
MSDS N/A Flash Point 384.7±32.9 °C

 Use of Radezolid


Radezolid is a novel oxazolidinone antibiotic agent.

 Names

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

 Radezolid Biological Activity

Description Radezolid is a novel oxazolidinone antibiotic agent.
Related Catalog
In Vitro Radezolid MICs are systematically equal to or lower (up to 3 log2 dilutions) than those of linezolid for all linezolid-susceptible strains, with an 8-fold difference for the linezolid-resistant strains. Radezolid shows a greater potency than linezolid, independent of the bacteria tested, when concentrations are expressed on a weight (mg/L) basis. Radezolid shows an improved potency compared to that of linezolid when concentrations are expressed on a weight (mg/L) basis[1]. Radezolid and TR-700 perform well against 3-copy G2447T, G2576T, and G2576T/T2571C mutants[2].
Cell Assay Antibiotic accumulation is determined following the general procedure, and the cellular content of [14C]radezolid is assayed in cell lysates by liquid scintillation counting (lowest limit of detection, 0.003 mg/liter; linear response between 0.01 and 0.78 mg/liter; R2=0.999). All cell drug contents are expressed by reference to the total cell protein content and converted into apparent total cell concentrations using a conversion factor of 5 μL per mg of cell protein. 
References

[1]. Lemaire S, et al. Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.

[2]. Locke JB, et al. Structure-activity relationships of diverse oxazolidinones for linezolid-resistant Staphylococcus aureus strains possessing the cfr methyltransferase gene or ribosomal mutations. Antimicrob Agents Chemother. 2010 Dec;54(12):5337-43.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 712.5±60.0 °C at 760 mmHg
Molecular Formula C22H23FN6O3
Molecular Weight 438.455
Flash Point 384.7±32.9 °C
Exact Mass 438.181580
PSA 112.24000
LogP 2.28
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.612

 Synthetic Route

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Radezolid Structure

Radezolid

CAS#:869884-78-6

Literature: US2010/234615 A1, ; Page/Page column 35 ;

 Synonyms

RX-1741
N-{[(5S)-3-(2-Fluoro-4'-{[(1H-1,2,3-triazol-4-ylmethyl)amino]methyl}-4-biphenylyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide
Radezolid
UNII-53PC6LO35W
RX-103
Acetamide, N-[[(5S)-3-[2-fluoro-4'-[[(1H-1,2,3-triazol-5-ylmethyl)amino]methyl][1,1'-biphenyl]-4-yl]-2-oxo-5-oxazolidinyl]methyl]-