jm000018k_si_001.pdf (58.91 kB)
Hydroxamic Acid Derivatives as Potent Peptide Deformylase Inhibitors and Antibacterial Agents
journal contribution
posted on 2000-05-20, 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 SpecklinLow-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.
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Mycoplasma pneumoniaeselectivityDerivativesulfonylPotent Peptide Deformylase InhibitorsHaemophilus influenzaeChlamydia pneumoniaeAntibacterialEscherichia coli peptide deformylasebacteriasulfinylhydroxamic acid derivativestract infectionspathogenMoraxella catarrhalisagentcompoundPDFintracellular concentrationsHydroxamicAgentresistance developmentinhibitor
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