(S)-Tedizolid - CAS 1431699-67-0
Catalog number: 1431699-67-0
Category: Inhibitor
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Molecular Formula:
C17H15FN6O3
Molecular Weight:
370.34
COA:
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Targets:
Antibacterial
Description:
Antibacterial oxazolidinone against gram-positive species
Purity:
>98%
Synonyms:
(S)-3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
MSDS:
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InChIKey:
XFALPSLJIHVRKE-LBPRGKRZSA-N
InChI:
InChI=1S/C17H15FN6O3/c1-23-21-16(20-22-23)15-5-2-10(7-19-15)13-4-3-11(6-14(13)18)24-8-12(9-25)27-17(24)26/h2-7,12,25H,8-9H2,1H3/t12-/m0/s1
Canonical SMILES:
CN1N=C(N=N1)C2=NC=C(C=C2)C3=C(C=C(C=C3)N4CC(OC4=O)CO)F
1.Stability of Crushed Tedizolid Phosphate Tablets for Nasogastric Tube Administration.
Kennedy G1, Osborn J2, Flanagan S3, Alsayed N4, Bertolami S5. Drugs R D. 2015 Dec;15(4):329-33. doi: 10.1007/s40268-015-0108-6.
Tedizolid phosphate is approved for the treatment of acute bacterial skin and skin structure infections. To determine whether the expected dose of tedizolid phosphate can be delivered via nasogastric tube in patients who have difficulty swallowing and in whom venous access is not suitable, this in vitro study evaluated the recovery of tedizolid phosphate 200-mg tablets after crushing, dispersion in water, and passage through a nasogastric tube. To analyze the chemical stability of the crushed tablet dispersed in water, the aqueous preparation was assayed initially after dispersion and again after 4 h at room temperature. Recovery of tedizolid phosphate after the crushed tablets were dispersed in water and passed through nasogastric tubes ranged from 92.5 to 97.1 %, which is within the specified acceptance criteria of 90 to 110 %. There was no significant change in recovery values after 4 h of storage at room temperature (93.9 % initially and 94.
2.In Vitro Activities of Tedizolid and Linezolid against Gram-Positive Cocci Associated with Acute Bacterial Skin and Skin Structure Infections and Pneumonia.
Chen KH1, Huang YT2, Liao CH2, Sheng WH3, Hsueh PR4. Antimicrob Agents Chemother. 2015 Oct;59(10):6262-5. doi: 10.1128/AAC.00390-15. Epub 2015 Jul 27.
Tedizolid is a novel, expanded-spectrum oxazolidinone with potent activity against a wide range of Gram-positive pathogens. A total of 425 isolates of Gram-positive bacteria were obtained consecutively from patients with acute bacterial skin and skin structure infections (ABSSSIs) or pneumonia. These isolates included methicillin-susceptible Staphylococcus aureus (MSSA) (n = 100), methicillin-resistant Staphylococcus aureus (MRSA) (n = 100), Streptococcus pyogenes (n = 50), Streptococcus agalactiae (n = 50), Streptococcus anginosus group (n = 75), Enterococcus faecalis (n = 50), and vancomycin-resistant enterococci (VRE) (Enterococcus faecium) (n = 50). The MICs of tedizolid and linezolid were determined by the agar dilution method. Tedizolid exhibited better in vitro activities than linezolid against MSSA (MIC90s, 0.5 versus 2 μg/ml), MRSA (MIC90s, 0.5 versus 2 μg/ml), S. pyogenes (MIC90s, 0.5 versus 2 μg/ml), S. agalactiae (MIC90s, 0.5 versus 2 μg/ml), Streptococcus anginosus group (MIC90s, 0.
3.In vitro activity of Tedizolid phosphate against multidrug-resistant Streptococcus pneumoniae isolates from Asian countries.
Baek JY1, Kang CI2, Kim SH3, Ko KS4, Chung DR3, Peck KR5, Hsueh PR6, Thamlikitkul V7, So TM8, Lee NY9, Song JH3; ANSORP Study Group. Diagn Microbiol Infect Dis. 2016 Mar 2. pii: S0732-8893(16)30038-4. doi: 10.1016/j.diagmicrobio.2016.02.022. [Epub ahead of print]
Tedizolid phosphate is a second-generation oxazolidinone prodrug that is potential activity against a wide range of Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicillin-resistant streptococci, and vancomycin-resistant enterococci. The in vitro activity of tedizolid and other comparator agents against multidrug-resistant (MDR) pneumococci from various Asian countries were evaluated. Of the S. pneumoniae clinical pneumonia isolates collected during 2008 and 2009 from 8 Asian countries (Korea, Taiwan, Thailand, Hong Kong, Vietnam, Malaysia, Philippines, and Sri Lanka), 104 isolates of MDR pneumococci were included in this study. Antimicrobial susceptibility testing for 18 antimicrobial agents was performed by broth microdilution method. Tedizolid was highly active against pneumococci. All isolates tested were inhibited at a tedizolid minimum inhibitory concentration (MIC) value of ≤0.25μg/ml (ranged from ≤0.
4.Evaluation of tedizolid against Staphylococcus aureus and enterococci with reduced susceptibility to vancomycin, daptomycin or linezolid.
Barber KE1, Smith JR1, Raut A1, Rybak MJ2. J Antimicrob Chemother. 2016 Jan;71(1):152-5. doi: 10.1093/jac/dkv302. Epub 2015 Oct 16.
OBJECTIVES: Tedizolid displays potent activity against Gram-positive pathogens. In vitro studies against clinical isolates of Staphylococcus aureus and enterococci demonstrated improved tedizolid activity over linezolid. However, this is not well-characterized against a large collection of resistant isolates, including vancomycin-intermediate S. aureus (VISA), heterogeneous VISA (hVISA), daptomycin-non-susceptible (DNS) S. aureus, linezolid-resistant (LR) S. aureus and VRE. Therefore, our objective was to determine tedizolid activity versus other agents, against MRSA and VRE with various resistance phenotypes.
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CAS 1431699-67-0 (S)-Tedizolid

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