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Bioorg Med Chem Lett. 2016 Jul 1;26(13):3148-3152. doi: 10.1016/j.bmcl.2016.04.086. Epub 2016 Apr 30.

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

Author information

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: jhkang@ildong.com.

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

PMID:
27173797
DOI:
10.1016/j.bmcl.2016.04.086
[Indexed for MEDLINE]

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