Ceftezole Sodium is the sodium salt of Cefezole. Ceftezole is a first-generation cephalosporin with broad-spectrum antibacterial activity. It is closely related to Cefazolin in chemical structure. It is alpha-glucosidase inhibitor with anti-diabetic properties.
| Application | Using high-throughput screening, researchers found that Cefezole exhibited potent alpha-glucosidase inhibitory activity. Glycosidase inhibitors are tools for studying the mechanism of action of glycosidases and are also potential therapeutic agents for diabetes. In vitro, it was an reversible and noncompetitive inhibitor of yeast alpha-glucosidase. Using a streptozotocin-induced in vivo diabetic mouse model, blood glucose levels decreased. Results suggest that this compound may be a useful anti-diabetic compound (Lee et al, 2007). |
| Mechanism of Action | Like β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases. |
| Spectrum | Broad-spectrum, effective against Gram-positive and Gram-negative species. |
| Microbiology Applications | Based on a study of 52 clinical isolates, authors found that Ceftezole resistance in Bacterioides fragilis may be due to a decreased affinity for PBP3 (Yotsuji et al, 1988) |
| Molecular Formula | C13H11N8O4S3 • Na |
| References | Georgopapadakou, NH (1992) Mechanisms of action of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines in Escherichia Coli. Antimicrob. Agents Chemother 37(3): 559-565 Lee D et al (2007) Cefezole, a cephem antibiotic, is an a-glucosidase inhibitorwith in vivo anti-diabetic activity. Intl. J. Molec. Med. 20(3):379-383. Nishida M et al (1976) In vitro and in vivo evaluation of Ceftezole, a new cephalosporin derivative. Antimicrob. Agents. Chemother. 10 (1) 1-13 PMID 825020 Yotsuji A et al (1988) Mechanism of action of cephalosporins and resistance caused by decreased affinity for penicillin-binding proteins in Bacteroides fragilis. Antimicrob. Agents Chemother. 32 (12):1848-1853 PMID 3266730 |
