Xiao Yong Sheng, Zhang Bo, Zhang Mei, Guo Zhi Kai, Deng Xin Zhao, Shi Jing, Li Wei, Jiao Rui Hua, Tan Ren Xiang, Ge Hui Ming
State Key Laboratory of Pharmaceutical Biotechnology, Institute of Functional Biomolecules, School of Life Sciences, Nanjing University, 163 Xianlin Avenue, Nanjing 210046, China.
Org Biomol Chem. 2017 May 10;15(18):3909-3916. doi: 10.1039/c7ob00614d.
Cultivation of locust associated rare actinobacteria, Amycolatopsis sp. HCa4, has provided five unusual macrolactams rifamorpholines A-E. Their structures were determined by interpretation of spectroscopic and crystallographic data. Rifamorpholines A-E possess an unprecedented 5/6/6/6 ring chromophore, representing a new subclass of rifamycin antibiotics. The biosynthetic pathway for compounds 1-5 involves a key 1,6-cyclization for the formation of the morpholine ring. Compounds 2 and 4 showed potent activities against methicillin-resistant Staphylococcus aureus (MRSA) with MICs of 4.0 and 8.0 μM, respectively.
与蝗虫相关的稀有放线菌——拟无枝酸菌属菌株HCa4的培养，产生了五种不同寻常的大环内酰胺类化合物利福吗啉A - E。通过对光谱和晶体学数据的解析确定了它们的结构。利福吗啉A - E具有前所未有的5/6/6/6环发色团，代表了利福霉素抗生素的一个新亚类。化合物1 - 5的生物合成途径涉及形成吗啉环的关键1,6 - 环化反应。化合物2和4对耐甲氧西林金黄色葡萄球菌（MRSA）显示出强效活性，其最低抑菌浓度（MIC）分别为4.0和8.0 μM。
