title: Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
abstract: The synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives are reported. The antibacterial activities of these derivatives were evaluated to discover SAR at P(1') and P(3') positions, and most of these derivatives exhibit better in vitro antibacterial activity than existing drugs against drug-resistant clinical isolates including MRSA, PRSP, and Haemophilus influenzae.
authors.affiliation: Institute of Drug Discovery and Development, Department of Chemistry, East China Normal University, Shanghai, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Shi
authors.forename: Haikun
authors.initials: H
authors.lastname: Ma
authors.forename: Yuejiao
authors.initials: Y
authors.lastname: Duan
authors.forename: Kelly
authors.initials: K
authors.lastname: Aubart
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Fang
authors.forename: Rimma
authors.initials: R
authors.lastname: Zonis
authors.forename: Liping
authors.initials: L
authors.lastname: Yang
authors.forename: Wenhao
authors.initials: W
authors.lastname: Hu
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006193:Haemophilus influenzae / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D011759:Pyrrolidines; D000581:Amidohydrolases; C084507:peptide deformylase; C032519:pyrrolidine