| Identification | Back Directory | [Name]
posizolid | [CAS]
252260-02-9 | [Synonyms]
AZD2563
AZD5847
AZD-5847
AZD-2563
posizoli
AZD 2563
AZD 5847
posizolid
Posizolid-13C2D4
AZD-2563, Posizolid
posizolid ISO 9001：2015 REACH
(5R)-3-[4-[1-[(2S)-2,3-Dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)methyl]-2-oxazolidinone
(5R)-3-[4-[1-[(2S)-2,3-dihydroxypropanoyl]-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluorophenyl]-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolidin-2-one
2-Oxazolidinone, 3-[4-[1-[(2S)-2,3-dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)methyl]-, (5R)-
Posizolid,(5R)-3-[4-[1-[(2S)-2,3-Dihydroxy-1-oxopropyl]-1,2,3,6-tetrahydro-4-pyridinyl]-3,5-difluorophenyl]-5-[(3-isoxazolyloxy)Methyl]-2-oxazolidinone | [Molecular Formula]
C21H21F2N3O7 | [MDL Number]
MFCD27987906 | [MOL File]
252260-02-9.mol | [Molecular Weight]
465.407 |
| Hazard Information | Back Directory | [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.
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| 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.
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| [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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