title: Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
abstract: We have previously reported amidopiperidine derivatives as a novel peptide deformylase (PDF) inhibitor and evaluated its antibacterial activity against Gram-positive bacteria, but poor pharmacokinetic profiles have resulted in low efficacy in in vivo mouse models. In order to overcome these weaknesses, we newly synthesized aminopiperidine derivatives with remarkable antimicrobial properties and oral bioavailability, and also identified their in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae (PRSP).
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Hee-Yeol
authors.initials: HY
authors.lastname: Lee
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Kyung-Mi
authors.initials: KM
authors.lastname: An
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Juyoung
authors.initials: J
authors.lastname: Jung
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Je-Min
authors.initials: JM
authors.lastname: Koo
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Jeong-Geun
authors.initials: JG
authors.lastname: Kim
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Jong-Min
authors.initials: JM
authors.lastname: Yoon
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Myong-Jae
authors.initials: MJ
authors.lastname: Lee
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: HyeonSoo
authors.initials: H
authors.lastname: Jang
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Hong-Sub
authors.initials: HS
authors.lastname: Lee
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
authors.forename: Soobong
authors.initials: S
authors.lastname: Park
authors.affiliation: Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea. Electronic address: jhkang@ildong.com.
authors.forename: Jae-Hoon
authors.initials: JH
authors.lastname: Kang
mesh_terms: D000284:Administration, Oral; D000581:Amidohydrolases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000201:enzymology; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D010880:Piperidines; D000581:Amidohydrolases; C084507:peptide deformylase
keywords: Aminopiperidine; Antibacterial; Gram-positive; Peptide deformylase; Resistant