C. Apfel et al., Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents, J MED CHEM, 43(12), 2000, pp. 2324-2331
Low-molecular-weight beta-sulfonyl- and beta-sulfinylhydroxamic acid deriva
tives have been synthesized and found to be potent inhibitors of Escherichi
a coli peptide deformylase (PDF). Most of the compounds synthesized and tes
ted displayed antibacterial activities that cover several pathogens found i
n respiratory tract infections, including Chlamydia pneumoniae, Mycoplasma
pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. The potentia
l of these compounds as antibacterial agents is discussed with respect to s
electivity, intracellular concentrations in bacteria, and potential for res
istance development.