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

详细信息    查看全文

• 作者：Hee-Yeol Lee ; Kyung-Mi An ; Juyoung Jung ; Je-Min Koo ; Jeong-Geun Kim ; Jong-Min Yoon ; Myong-Jae Lee ; HyeonSoo Jang ; Hong-Sub Lee ; Soobong Park ; Jae-Hoon Kang ; ^{jhkang@ildong.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Peptide deformylase ; Antibacterial ; Gram-positive ; Resistant ; Aminopiperidine
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 July 2016
• 年：2016
• 卷：26
• 期：13
• 页码：3148-3152
• 全文大小：1228 K

文摘

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).