856866-72-3

856866-72-3 structure

Name: Tedizolid
Chemical Name: tedizolid
CAS Number: 856866-72-3
Molecular Formula: C₁₇H₁₅FN₆O₃
Molecular Weight: 370.338
Catalog: API Synthetic anti-infective drugs Antifungal drugs
Create Date: 2018-08-21 16:00:39
Modify Date: 2024-01-02 18:45:30
Tedizolid is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.

Name	tedizolid
Synonyms	(5R)-3-{3-Fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl}-5-(hydroxymethyl)-1,3-oxazolidin-2-one Torezolid TR-701 (5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one TR-700 (R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one Tedizolid [USAN:INN] 2-Oxazolidinone, 3-[3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl]phenyl]-5-(hydroxymethyl)-, (5R)- UNII:97HLQ82NGL Tedizolid (5R)-3-{3-fluoro-4-[6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl]phenyl}-5-(hydroxymethyl)-2-oxazolidinone

Description	Tedizolid is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Related Catalog	Signaling Pathways >> Anti-infection >> Bacterial Research Areas >> Infection
In Vitro	Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP[1].
In Vivo	For mice infected with PSSP type III, the 100% survival rate is achieved with tedizolid phosphate at a minimum total daily dose of 10 mg/kg. Lungs of infected mice treated with tedizolid phosphate show less severe inflammation and edema, as indicated by the mean scores for inflammation and edema[1].
Animal Admin	To induce a systemic S. pneumoniae infection, male ICR mice (weight, 18 to 20 g) are inoculated intraperitoneally with 1 of 4 PRSP isolates (DR9, DR10, DR11, or DR14) suspended in 10% mucin. The suspension contained sufficient bacteria to kill 100% of untreated control mice. At 1 h postinfection, mice receives a single dose of either tedizolid phosphate or linezolid, and survival is assessed daily for 7 days postinfection. Treatments are delivered both orally and intravenously at each of four doses (40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg), with 8 mice per group defined by dose, delivery method, and infecting strain. The 50% effective dose (ED50), i.e., the dose allowing survival of 50% of the infected mice, is calculated for each delivery route using probit analysis.
References	[1]. Choi S, et al. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19.

Density	1.6±0.1 g/cm3
Boiling Point	614.5±65.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₅FN₆O₃
Molecular Weight	370.338
Flash Point	325.4±34.3 °C
Exact Mass	370.118958
PSA	106.26000
LogP	1.56
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.725

HS Code	29339900

1220910-89-3

60456-26-0

~84%

856866-72-3

Literature: TRIUS THERAPEUTICS; COSTELLO, Carrie, A.; SIMSON, Jaqueline, A.; DUGUID, Robert, J.; PHILLIPSON, Douglas Patent: WO2010/42887 A2, 2010 ; Location in patent: Page/Page column 19-20 ;

624-28-2

856866-72-3

Literature: European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

97483-77-7

856866-72-3

Literature: European Journal of Medicinal Chemistry, , vol. 46, # 4 p. 1027 - 1039

Precursor 4
1220910-89-3 60456-26-0 624-28-2 97483-77-7
DownStream 0

856866-72-3	1092939-15-5
1431699-67-0	1256966-04-7
856867-55-5	1700656-53-6
1239662-45-3	1239662-43-1
1239662-49-7	1239662-44-2