Synthesis and In Vitro Antibacterial Activity of (2S)-N-(Substitutedphenyl)-1-[(2R)-2-[(Formylhydroxyamino)Methyl]-1-Oxohexyl]-2-Pyrrolidinecarboxamides as Potential Peptide Deformylase Inhibitors

摘要

Gram-positive organisms have re-emerged as the major hospital pathogens, which make the unmet medical needs for antibacterial therapy even worse. In searching for potent agents against Gram-positive pathogens, novel (2S)-N-(substitutedphenyl)-1-[(2R)-2-[(formylhydroxyamino)methyl]-1-oxo hexyl]-2-pyrrolidinecarboxamides, analogues of peptide deformylase inhibitor LBM-415 were designed, synthesized and evaluated for their antibacterial activities in vitro. Many of these compounds exhibited high potency against Gram-positive organisms compared with reference agent: LBM-415.