CAS 252260-02-9|Posizolid
Introduction：Basic information about CAS 252260-02-9|Posizolid, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Posizolid | ||
|---|---|---|---|
| CAS Number | 252260-02-9 | Molecular Weight | 465.404 |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 724.5±60.0 °C at 760 mmHg |
| Molecular Formula | C21H21F2N3O7 | Melting Point | / |
| MSDS | / | Flash Point | 392.0±32.9 °C |
Names
| Name | posizolid |
|---|---|
| Synonym | More Synonyms |
Posizolid BiologicalActivity
| Description | Posizolid (AZD2563), an oxazolidinone antibiotic, is developed by AstraZeneca for the study of bacterial infections. Posizolid shows very good anti-mycobacterial activity[1]. |
|---|---|
| Related Catalog | Research Areas >>InfectionSignaling Pathways >>Others >>Others |
| Target | Posizolid shows very good anti-mycobacterial activity[1]. |
| In Vitro | Posizolid is determined the activity of against 250 highly resistant pneumococci and 267 drug-susceptible isolates. Posizolid MICs for 50 and 90% of the strains tested are 1 and 2 μg/ml and 0.5 and 1 μg/ml, respectively, for the two isolate groups[2]. |
| 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. |
| References | [1]. Kumar D, et al. The anti-tuberculosis agents under development and the challenges ahead. Future Med Chem. 2015;7(15):1981-2003. [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. [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. |
Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 724.5±60.0 °C at 760 mmHg |
| Molecular Formula | C21H21F2N3O7 |
| Molecular Weight | 465.404 |
| Flash Point | 392.0±32.9 °C |
| Exact Mass | 465.134766 |
| PSA | 125.57000 |
| LogP | 1.34 |
| Vapour Pressure | 0.0±2.5 mmHg at 25°C |
| Index of Refraction | 1.596 |
| InChIKey | HBUJYEUPIIJJOS-PBHICJAKSA-N |
| SMILES | O=C(C(O)CO)N1CC=C(c2c(F)cc(N3CC(COc4ccon4)OC3=O)cc2F)CC1 |
Synonyms
| (5R)-3-(4-(1-((2S)-2,3-Dihydroxypropanoyl)-1,2,3,6-tetrahydro-4-pyridyl)-3,5-difluorophenyl)-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolan-2-one |
| (5R)-3-(4-(1-((2S)-2,3-Dihydroxypropanoyl)-1,2,3,6-tetrahydro-4-pyridyl)-3,5-difluorophenyl)-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolidin-2-one |
| Posizolid |
| (5R)-3-(4-{1-[(2S)-2,3-Dihydroxypropanoyl]-1,2,3,6-tetrahydropyridin-4-yl}-3,5-difluorophenyl)-5-[(1,2-oxazol-3-yloxy)methyl]-1,3-oxazolidin-2-one |
| AZD2563 |
| (5R)-3-(4-{1-[(2S)-2,3-Dihydroxypropanoyl]-1,2,3,6-tetrahydro-4-pyridinyl}-3,5-difluorophenyl)-5-[(1,2-oxazol-3-yloxy)methyl]-1,3-oxazolidin-2-one |
| (5R)-3-(4-{1-[(2S)-2,3-Dihydroxypropanoyl]-1,2,3,6-tetrahydro-4-pyridyl}-3,5-difluorophenyl)-5-(1,2-oxazol-3-yloxymethyl)-1,3-oxazolan-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 [INN] |
