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  • Title: Synthesis and antimicrobial activity of β-carboline derivatives with N2-alkyl modifications.
    Author: Suzuki K, Nomura I, Ninomiya M, Tanaka K, Koketsu M.
    Journal: Bioorg Med Chem Lett; 2018 Sep 15; 28(17):2976-2978. PubMed ID: 30001916.
    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.
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