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Updated: May 31, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and antibacterial activity of C2-symmetric binaphthyl scaffolded amino acid derivatives
Mark Robertson1, John B Bremner, Jonathan Coates
1School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia.
Abstract:
The synthesis of eleven novel antibacterial agents is reported. The structures are based on a C(2)-symmetric binaphthyl scaffold which holds two identical chains consisting of a short linker, a basic amino acid and a small hydrophobic side chain. Antibacterial activity is revealed for a number of derivatives down to an MIC of 2 μg/mL (2 μM) against Staphylococcus aureus--comparable to vancomycin, and an MIC of 31 μg/mL (31 μM) against some vancomycin-resistant enterococcal strains.
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