Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033 (Japan).
Angew Chem Int Ed Engl. 2015 Jan 26;54(5):1556-60. doi: 10.1002/anie.201410270. Epub 2014 Dec 11.
Lysocin E, a macrocyclic peptide, exhibits potent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) through a novel mechanism. The first total synthesis of lysocin E was achieved by applying a full solid-phase strategy. The developed approach also provides rapid access to the enantiomeric, epimeric, and N-demethylated analogues of lysocin E. Significantly, the antibacterial activity of the unnatural enantiomer was comparable to that of the natural isomer, suggesting the absence of chiral recognition in its mode of action.
赖氨酸 E 是一种环状肽，通过一种新的机制对耐甲氧西林金黄色葡萄球菌（MRSA）表现出强大的抗菌活性。赖氨酸 E 的首次全合成是通过应用完全固相策略实现的。所开发的方法还为赖氨酸 E 的对映体、差向异构体和 N-去甲基类似物提供了快速途径。值得注意的是，非天然对映异构体的抗菌活性与天然异构体相当，这表明在其作用模式中不存在手性识别。
