165800-04-4 Usage
Uses
Different sources of media describe the Uses of 165800-04-4 differently. You can refer to the following data:
1. Antibacterial.
2. Eperezolid is an antimicrobial.
Biological Activity
mic50: 0.5, 1.0, 2.0, 1.0, 16.0 and 2.0 mg/l for pcptostreptococcus, propionibacterium acnes, ciostridium pefringens, clostridium dijiicile, bactrroidesjagilis, and fusobacterium, respectivleyanaerobic bacteria are a common cause of serious infections. anaerobic species which predominate in clinical infections include the bacteroides fragilis group, clostridium spp. and peptostreptococcus spp. the oxazolidinones are a novel class of synthetic antimicrobials inhibiting the initiation of protein synthesis. two compounds of this class, eperezolid and linezolid have been shown to inhibit enterococcus faecalis and enterococcus faecium.
in vitro
ninety per cent of all tested propionibacterium acnes (30 strains), peptostreptococccuj spp. (50 strains), c. perjringens (50 strains) and c. dficile (50 strains) were inhibited by <2 mg/l eperezolid. linezolid showed higher activity (mic90 4.0 mg/l) against b. jragilis (100 strains) compared to eperezolid (mic90 16 mg/l) [1].
in vivo
the in vivo effectiveness of eperezolid and linezolid against one strain each of enterococcus faecalis and vancomycin-resistant enterococcus faecium was examined in a rat intraabdominal abscess model. eperezolid was ineffective at doses of 25 mg/kg of body weight twice daily for the reductions in abscess bacterial density for e. faecalis. against e. faecium infections, intravenous eperezolid was effective, reducing densities approximately 2 log10 cfu/g [2].
references
[1] edlund c, oh h, nord ce. in vitro activity of linezolid and eperezolid against anaerobic bacteria. clin microbiol infect. 1999;5(1):51-53.[2] schülin t, thauvin-eliopoulos c, moellering rc jr, eliopoulos gm. activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to enterococcus faecalis or vancomycin-resistant enterococcus faecium. antimicrob agents chemother. 1999;43(12):2873-6.[3] schaadt rd, batts dh, daley-yates pt, pawsey sd, stalker dj, zurenko ge. serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid. diagn microbiol infect dis. 1997;28(4):201-4.
Check Digit Verification of cas no
The CAS Registry Mumber 165800-04-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,5,8,0 and 0 respectively; the second part has 2 digits, 0 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 165800-04:
(8*1)+(7*6)+(6*5)+(5*8)+(4*0)+(3*0)+(2*0)+(1*4)=124
124 % 10 = 4
So 165800-04-4 is a valid CAS Registry Number.
InChI:InChI=1/C18H23FN4O5/c1-12(25)20-9-14-10-23(18(27)28-14)13-2-3-16(15(19)8-13)21-4-6-22(7-5-21)17(26)11-24/h2-3,8,14,24H,4-7,9-11H2,1H3,(H,20,25)/t14-/m0/s1
165800-04-4Relevant articles and documents
A convenient synthesis of oxazolidinone derivatives linezolid and eperezolid from (S)-glyceraldehyde acetonide
Guangyu, Xu,Yi, Zhou,Chunhao, Yang,Yuyuan, Xie
, p. 316 - 319 (2008/09/19)
A new convenient method for the synthesis of oxazolidinone antibacterials Linezolid and Eperezolid from readily available (S)-glyceraldehyde acetonide was developed. The key steps include reductive amination of arylamine and (S)-glyceraldehyde acetonide in the presence of NaBH4 and 4 A sieve, followed by hydrolysis and regioselective cyclization.
Treating infections by administration of oxazolidinones
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, (2008/06/13)
Disclosed is a method of treating ear infections, soft-tissue infections, acne, or cellulitis in a mammal in need thereof comprising administration of Oxazolidinone in a pharmaceutical formulation or composition to the skin of the mammal at a site proximal to the site of the infection to deliver a pharmaceutically-effective amount of Oxazolidinone to the infection to have a concentration of the Oxazolidinone at the site of infection of about 0.5 to about 4 μg/ml, provided that the application for administration is not directly to the site of the infection.
TOPICAL ADMINISTRATION OF OXAZOLIDINONES FOR TRANSDERMAL DELIVERY
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, (2008/06/13)
Disclosed is a method of treating a non-topical infection selected from the group consisting of ear infections, skin and soft tissue infections, acne, infected wounds, bacteremia, in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of a pharmaceutical formulation containing a transdermally effective amount of an OXAZOLIDINONE.
