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posizolid

Product Nameposizolid
CAS252260-02-9
MFC21H21F2N3O7
MW465.407
EINECS
MOL File252260-02-9.mol

Chemical Properties

Boiling point	724.5±60.0 °C(Predicted)
Density	1.491
pka	12.79±0.20(Predicted)

Usage And Synthesis

Uses

Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity[1].

in vivo

AZD5847 DSP (AZD2563 is prodrug) could not be detected in plasma 5 min after oral administration, suggesting rapid conversion of the prodrug to the parent molecule.
In PK analysis, AZD5847(5 mg/kg) shows a low clearance (4.7 ml/min/kg) and volume of distribution (0.5 liter/kg) in mice, the half-life is 1.3 h^[3].

Animal Model:	Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g^[3].
Dosage:	3, 10, 30, 100, 300, 600, and 900 mg/kg
Administration:	oral; collect blood samples at 5 min, 10 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 24 h
Result:	AZD5847 DSP can’t be detected in plasma 5 min.

Animal Model:	Male BALB/c mice, aged 6 to 8 weeks, 30 to 40 g^[3].
Dosage:	250 mg/kg
Administration:	oral; collect blood and BAL fluid samples at 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, and 48 h
Result:	AZD5847(5 mg/kg) shows a low clearance (4.7 ml/min/kg) and volume of distribution (0.5 liter/kg) in mice, the half-life is 1.3 h.

IC 50

Oxazolidinone

References

[1] Kumar D, et al. The anti-tuberculosis agents under development and the challenges ahead. Future Med Chem. 2015;7(15):1981-2003. DOI:10.4155/fmc.15.128
[2] Baum SE, et al. Comparative activities of the oxazolidinone AZD2563 and linezolid against selected recent North American isolates of Streptococcus pneumoniae. Antimicrob Agents Chemother. 2002;46(9):3094-3095. DOI:10.1128/AAC.46.9.3094-3095.2002
[3] Balasubramanian V, et al. Pharmacokinetic and pharmacodynamic evaluation of AZD5847 in a mouse model of tuberculosis. Antimicrob Agents Chemother. 2014;58(7):4185-4190. DOI:10.1128/AAC.00137-14

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