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Updated: Jan 31, 2026

Curation of Computational Chemical Libraries Demonstrated with Alpha-Amino Acids
Published on: April 13, 2022
Multicomponent Approach to a Library of N-Substituted γ-Lactams
Josipa Suć Sajko1, Vanja Ljoljić Bilić2, Ivan Kosalec2
1Ruđer Bošković Institute , Division of Organic Chemistry and Biochemistry , Bijenička cesta 54 , 10000 Zagreb , Croatia.
Abstract:
The γ-lactam motif is often found in naturally occurring compounds with diverse biological activities. We prepared a 28-member library of N-substituted γ-lactams following a single-pot, three-component Ugi reaction comprising bifunctional building block, l-glutamic acid methyl ester. The reaction tolerates structurally diverse carbonyl and isocyanide components providing a robust access to functionalized γ-lactams. Antimicrobial susceptibility testing, including agar well diffusion assay, serial microdilution broth assay, and antibiofilm activity testing, identified a potent compound with antibiofilm activity against Staphylococcus aureus ATCC 6538.
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