Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors

Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli   PDF (KI∗=4.4nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC = 2–4 μg/mL).

Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli   PDF (KI∗=4.4nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC = 2–4 μg/mL).Figure optionsDownload as PowerPoint slide