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Multicomponent approach to a library of N-substituted γ-lactams.

Research paper by Josipa J Suć Sajko, Vanja V Ljoljić Bilić, Ivan I Kosalec, Ivanka I Jeric

Indexed on: 20 Dec '18Published on: 20 Dec '18Published in: ACS Combinatorial Science



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. 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 S. aureus ATCC 6538..