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Synthesis and antimicrobial activity of β-carboline derivatives with N2-alkyl modifications |
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| Authors: | Kenji Suzuki Itsuki Nomura Masayuki Ninomiya Kaori Tanaka Mamoru Koketsu |
| Institution: | 1. Department of Materials Science and Technology, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan;2. Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan;3. Division of Anaerobe Research, Life Science Research Center, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan;4. United Graduate School of Drug Discovery and Medicinal Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan |
| Abstract: | β-Carbolines constitute a vast group of indole alkaloids and exhibit various biological actions. The objective of this study was to investigate the structure–activity relationships of β-carboline derivatives on in vitro inhibitory effects against clinically relevant microorganisms. A series of β-carboline dimers and their N2-alkylated analogues were therefore prepared and evaluated for their antimicrobial effects. Among these, a dimeric 6-chlorocarboline N2-benzylated salt exerted potent activity against Staphylococcus aureus at MICs of 0.01–0.05?μmol/mL. Our work highlights that N1-N1 dimerization and N2-benzylation significantly enhanced the antimicrobial effects of compounds. |
| Keywords: | β-Carboline Antimicrobial effect Corresponding author at: Department of Chemistry and Biomolecular Science Faculty of Engineering Gifu University 1-1 Yanagido Gifu 501-1193 Japan |
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