The Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, U.K.
Department of Pharmaceutical Engineering, China Pharmaceutical University, Nanjing 211198, P. R. China.
J Org Chem. 2020 Oct 2;85(19):12393-12407. doi: 10.1021/acs.joc.0c01636. Epub 2020 Sep 17.
The synthesis, structural, and antibacterial evaluation of bicyclic tetramate derivatives of cysteine rendered hydrophilic with pendant heterocyclic substituents is reported; effective synthetic protocols and antibacterial activity for a small library of polar derivatives were found, and direct evidence for strong metal chelation in these systems was obtained. A computational study has developed a detailed understanding of the controlling factors of the key Dieckmann cyclization step.
报道了带有杂环取代基的亲水侧链的半胱氨酸双环四肽衍生物的合成、结构和抗菌评价；找到了有效合成方案和针对小部分极性衍生物的抗菌活性，并且在这些体系中获得了金属螯合的直接证据。一项计算研究深入了解了关键的狄克曼环化步骤的控制因素。
