Drug intelligence / Profile preview

ceftezole

Development stage
Unknown
Modality
Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Ceftezole is a semisynthetic first-generation cephalosporin antibiotic belonging to the beta-lactam class. It exhibits broad-spectrum antibacterial activity against many gram-positive and gram-negative bacteria, though it is not effective against Pseudomonas aeruginosa, Serratia marcescens, or Proteus vulgaris. Ceftezole acts by binding to and inactivating penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. These PBPs are transpeptidases essential for peptidoglycan biosynthesis; their inhibition disrupts cell wall synthesis, leading to bacterial cell lysis and death[1][3][5][8]. In addition to its antibacterial effects, ceftezole has demonstrated potent alpha-glucosidase inhibitory activity in vitro as a reversible non-competitive inhibitor[3][8]. Clinically, it is used for treating susceptible infections such as septicemia; respiratory, biliary or genitourinary tract infections; skin and skin structure infections; endocarditis; and for surgical prophylaxis[3][4].

Other names
cefetzolceftezole sodium
02

Targets

Sucrase-IsomaltasePBP (Penicillin-binding protein family)

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