Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria

  • Bioorg Med Chem Lett. 2016 Jul 1;26(13):3148-3152. doi: 10.1016/j.bmcl.2016.04.086.
Hee-Yeol Lee  1 ,  Kyung-Mi An  1 ,  Juyoung Jung  1 ,  Je-Min Koo  1 ,  Jeong-Geun Kim  1 ,  Jong-Min Yoon  1 ,  Myong-Jae Lee  1 ,  HyeonSoo Jang  1 ,  Hong-Sub Lee  1 ,  Soobong Park  1 ,  Jae-Hoon Kang  2
Affiliations
  • 1. Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea.
  • 2. Research Laboratories ILDONG Pharmaceutical Co. Ltd, 20, Samsung 1-ro 1-gil, Hwaseong-si, Gyeonggi-do 18449, Republic of Korea. Electronic address: [email protected].
PMID: 27173797 DOI: 10.1016/j.bmcl.2016.04.086
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).

Keywords
Aminopiperidine; Antibacterial; Gram-positive; Peptide deformylase; Resistant.
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