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Hydroxamic Acid Derivatives as Potent Peptide Deformylase Inhibitors and Antibacterial Agents

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journal contribution
posted on 20.05.2000, 00:00 authored by Christian Apfel, David W. Banner, Daniel Bur, Michel Dietz, Takahiro Hirata, Christian Hubschwerlen, Hans Locher, Malcolm G. P. Page, Wolfgang Pirson, Gérard Rossé, Jean-Luc Specklin
Low-molecular-weight β-sulfonyl- and β-sulfinylhydroxamic acid derivatives have been synthesized and found to be potent inhibitors of Escherichia coli peptide deformylase (PDF). Most of the compounds synthesized and tested displayed antibacterial activities that cover several pathogens found in respiratory tract infections, including Chlamydia pneumoniae, Mycoplasma pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. The potential of these compounds as antibacterial agents is discussed with respect to selectivity, intracellular concentrations in bacteria, and potential for resistance development.