A versatile approach for the synthesis of a diverse library of macrocyclic and medium-sized ring lactams is described. Up to three-sequential synthetic steps were used, starting with a conjugate addition/ring expansion cascade, followed by side-chain and ring elaboration steps. The library was tested for antibacterial activity against Staphylococcus aureus and Escherichia coli. Although no novel antibacterial agents were uncovered in this study, the utility of the approach to quickly generate diverse lactam libraries for bioassay is confirmed.
Synthesis of a macrocyclic and medium-sized ring lactam library using cascade ring expansion reactions
Selin Yilmaz,Haimei Zhou,Çağrı Özsan,Angelo Frei,Peter O'Brien,W. Unsworth
Published 2025 in Organic and biomolecular chemistry
ABSTRACT
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- Publication year
2025
- Venue
Organic and biomolecular chemistry
- Publication date
2025-08-19
- Fields of study
Medicine, Chemistry
- Identifiers
- External record
- Source metadata
Semantic Scholar, PubMed
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