July 7, 2019  |  

Rifamorpholines A-E, potential antibiotics from locust-associated actinobacteria Amycolatopsis sp. Hca4.

Authors: Xiao, Yong Sheng and Zhang, Bo and Zhang, Mei and Guo, Zhi Kai and Deng, Xin Zhao and Shi, Jing and Li, Wei and Jiao, Rui Hua and Tan, Ren Xiang and Ge, Hui Ming

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.

Journal: Organic & biomolecular chemistry
DOI: 10.1039/c7ob00614d
Year: 2017

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