The role of adjuvants in overcoming antibacterial resistance due to enzymatic drug modification

Abstract

Antibacterial resistance is a prominent issue with monotherapy often leading to treatment failure in serious infections. Many mechanisms can lead to antibacterial resistance including deactivation of antibacterial agents by bacterial...

Synergistic Antimicrobial Activity of Eugenol in Combination with Fosfomycin to Combat Escherichia coli and Potential Effect on Plasmid‐Mediated Fosfomycin Resistance Genes

“…The third mechanism involves Fosfomycin inactivation by enzymatic cleavage of the oxirane ring of the antibiotic or phosphorylation of the phosphonate group. Fosfomycin‐specific epoxide hydrolase (FosX), glutathione transferase (FosA), and L‐cysteine thiol transferase (FosB) are two of the several enzymes involved in opening the oxirane ring [30] …”

Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation

“…For more extensive descriptions of inhibitors of resistance to aminoglycosides, the reader is referred to other recent review articles. 28,29,60,61,63,64,[100][101][102][103][104][105][106]…”

Synthesis and inhibitory activity against MurA and MurZ enzymes of 4H-pyrano[2,3-d]pyrimidine–1H-1,2,3-triazole hybrid compounds having piperidine and morpholine rings

“…Peptidoglycan (PGN, or murein) is a polysaccharide consisting of amino acids, which is necessary to form a mesh-like peptidoglycan layer outside the plasma membrane of most bacteria. 1 Intact peptidoglycan is essential for bacterial survival, 2 therefore, the steps in peptidoglycan biosynthesis are considered to be important targets for the discovery of new antibacterial agents. 3 PGN is one of the classic drug targets, but remains a notable target in the design of compounds with antimicrobial activity.…”

“…Therefore, this is considered the basis in the design of MurA covalent inhibitors. 1,2,19 Many novel chemical scaffolds with similar inhibitory properties to fosfomycin against Mur enzymes have been produced. 6,7,11,14 Some of the most recently reported representative inhibitors are presented in Fig.…”