title: Synthesis and in vitro antibacterial activity of (2S)-N-(substitutedphenyl)-1-[(2R)-2-[(formylhydroxyamino)methyl]-1-oxohexyl]-2-pyrrolidinecarboxamides as potential peptide deformylase inhibitors.
abstract: 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-oxohexyl]-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.
authors.affiliation: State Key Laboratory of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, 1111 Zhongshanbeiyi Road, Shanghai 200437, China. zhenyulangg@hotmail.com
authors.forename: Zhenyu
authors.initials: Z
authors.lastname: Wang
authors.forename: Weicheng
authors.initials: W
authors.lastname: Zhou
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000581:Amidohydrolases / Q000037:antagonists & inhibitors*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry*
chemical_list: D000577:Amides; D000900:Anti-Bacterial Agents; C487638:NVP PDF 713; D010455:Peptides; D000581:Amidohydrolases; C084507:peptide deformylase