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Ceftaroline fosamil acetate

Names

[ CAS No. ]:
400827-55-6

[ Name ]:
Ceftaroline fosamil acetate

[Synonym ]:
ceftaroline fosamil acetate monohydrate
(6R,7R)-7-({(2Z)-2-(Ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl}amino)-3-{[4-(1-methyl-4-pyridiniumyl)-1,3-thiazol-2-yl]sulfanyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate acetate hydrate (1:1:1)
Ceftaroline fosamil acetate hydrate
(6R,7R)-7-[[(2Z)-2-ethoxyimino-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-3-[[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,acetate,hydrate
Ceftaroline fosamil acetate

Biological Activity

[Description]:

Ceftaroline fosamil hydrate acetate is a potent cephalosporin antibiotic. Ceftaroline fosamil hydrate acetate shows broad-spectrum activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative organisms. Ceftaroline fosamil hydrate acetate has anti-infective activity, and can be used for the research of complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP)[1][2][3].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vivo]

Ceftaroline fosamil hydrate acetate (s.c.) shows protective effects against experimental systemic infection caused by S. aureus N133 in mice, with ED50s of 1.60-2.37 mg/kg[1]. Ceftaroline fosamil hydrate acetate (10 mg/kg; s.c.) disappeares rapidly and converts smoothly into T-91825 in blood of rats and monkeys[1].

[References]

[1]. Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37.

[2]. Biek D, et al. Ceftaroline fosamil: a novel broad-spectrum cephalosporin with expanded anti-Gram-positive activity. J Antimicrob Chemother. 2010 Nov;65 Suppl 4:iv9-16.

[3]. Parish D, et al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H27N8O11PS4

[ Molecular Weight ]:
762.752

[ Exact Mass ]:
762.041992

[ PSA ]:
393.38000

[ LogP ]:
1.88460

Related Compounds