122841-12-7

Cefoselis is a new fourth-generation cephalosporin and was launched in Japan as a parenteral antibiotic for a variety of infections including Staphylococcus aureus (particularly the methicillin-resistant MRSA) and Pseudornonas aeruginosa. It can be prepared in 3 related ways, all using 2- pyrazolomethyl-3-cephem-4-carboxylic as the key intermediate. In preclinical studies, Cefolesis had better MIC50s than Ceftazidime against Streptococcus pneurnoniae or Staphflococcus aureus (methicillin-sensitive MSSA or resistant MRSA) and showed significant antibacterial activity against Citrobacter and Enterobacter.
Cefolesis is well tolerated in clinical studies, being eliminated mainly via glomerular filtration in humans.

Fujisawa (Japan)

antibiotic

ChEBI: Cefoselis sulfate is an azaheterocycle sulfate salt. It is functionally related to a member of cefoselis.

Wincef

[1] K OHTAKI. Cefoselis, a beta-lactam antibiotic, easily penetrates the blood-brain barrier and causes seizure independently by glutamate release.[J]. Journal of Neural Transmission, 2004, 111 12: 1523-1535. DOI:10.1007/s00702-004-0177-0. 
[2] PRZEMYSŁAW ZALEWSKI   Anna J  Judyta Cielecka Piontek. Stability of cefoselis sulfate in aqueous solutions[J]. Reaction Kinetics, Mechanisms and Catalysis, 2012, 108 2: 285-292. DOI:10.1007/s11144-012-0523-4.
[3] ZHU, D., et al., In vitro activities of cefoselis compared to β-lactams and other antibacterial agents aganst gram-positive and gram-negative clinical isolates. Chinese Journal of Infection and Chemotherapy, 2011. 4: p. 002.
[4] ANNA KING   Ian P  Linda Bethune. The Comparative In Vitro Activity of FK-037 (Cefoselis), a New Broad-Spectrum Cephalosporin[J]. Clinical Microbiology and Infection, 1995, 1 1: Pages 13-17. DOI:10.1111/j.1469-0691.1995.tb00018.x.