Josa-Culleré Laia, Towers Christopher, Willenbrock Frances, Macaulay Valentine M, Christensen Kirsten E, Moloney Mark G
Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford, OX1 3TA, UK.
Org Biomol Chem. 2017 Jun 27;15(25):5373-5379. doi: 10.1039/c7ob01148b.
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.
一项关于与γ-内酰胺稠合和螺环化的β-内酯形成的研究表明，在标准条件下，稠合体系优先形成，但只有当稠合体系的形成受阻时，螺环体系才能够得到，并且需要仔细优化反应条件。这些体系兼具弱抗菌活性和蛋白酶体抑制作用。
