Issue 25, 2017

Synthesis and bioactivity of fused- and spiro-β-lactone-lactam systems

Abstract

An investigation of the formation of fused- and spiro-β-lactone annulate to γ-lactams has shown that the fused systems are formed preferentially, under standard conditions, but that spiro systems are accessible only when the formation of the fused system is blocked and require careful optimisation of reaction conditions. These systems display both weak antibacterial activity and proteasome inhibition.

Graphical abstract: Synthesis and bioactivity of fused- and spiro-β-lactone-lactam systems

Supplementary files

Article information

Article type
Paper
Submitted
10 May 2017
Accepted
05 Jun 2017
First published
05 Jun 2017

Org. Biomol. Chem., 2017,15, 5373-5379

Synthesis and bioactivity of fused- and spiro-β-lactone-lactam systems

L. Josa-Culleré, C. Towers, F. Willenbrock, V. M. Macaulay, K. E. Christensen and M. G. Moloney, Org. Biomol. Chem., 2017, 15, 5373 DOI: 10.1039/C7OB01148B

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