Department of Chemistry, Scripps Research, 10550N. Torrey Pines Road, La Jolla, CA 92122, USA.
Department of Biology, Northeastern University, 360 Huntington Avenue, Boston, Ma 02115, USA.
Angew Chem Int Ed Engl. 2022 Aug 8;61(32):e202206183. doi: 10.1002/anie.202206183. Epub 2022 Jul 6.
A modular total synthesis of kibdelomycin is disclosed that should enable structure-activity relationship (SAR) studies of this interesting class of antibiotics. The route uses simple building blocks and addresses lingering questions about its structural assignment and relationship to amycolamicin, a recently described natural product reported to have a similar structure. Initial antibacterial assays reveal that both C-22 epimers (the N-glycosidic linkage) of the natural product have similar activity while structurally truncated analogs lose activity.
本文公开了一种卷曲霉素的模块化全合成方法，这将有助于对这类新型抗生素进行结构-活性关系（SAR）研究。该路线使用了简单的起始原料，并解决了有关其结构确定以及与 recently described natural product reported to have a similar structure 的amycolamicin 的关系的遗留问题。初步的抗菌活性测试表明，天然产物的 C-22 差向异构体（N-糖苷键）具有相似的活性，而结构截短的类似物则失去了活性。
