CHIR-090 is a very potent and tight-binding inhibitor of LpxC, which is a zinc-dependent amidase and present in almost all Gram-negative bacteria, and is a promising target for the development of novel antibiotic substances against multigrug-resistant Gram-negative bacteria. Its Ki value is 4.0 nM. It displays two-step time-dependent inhibition and kills a wide range of Gram-negative pathogens as effectively as ciprofloxacin or tobramycin. It has a different selectivity with the reported LpxC inhibitor L-161. It has excellent antibiotic activity against Pseudomonas aeruginosa and Escherichia coli by inhibiting LpxC orthologs at low nM concentrations. It is an excellent lead for the further development of new antibiotics targeting the lipid A pathway.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Infection | Antibacterial
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