Total synthesis and antimicrobial evaluation of natural albomycins against clinical pathogens

Zihua Lin, Xiaobo Xu, Sheng Zhao, Xiaohong Yang, Jian Guo, Qun Zhang, Chunmei Jing, Shawn Chen and Yun He ()
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Zihua Lin: Chongqing University
Xiaobo Xu: Chongqing University
Sheng Zhao: Chongqing University
Xiaohong Yang: Chongqing University
Jian Guo: Chongqing University
Qun Zhang: Children’s Hospital of Chongqing Medical University
Chunmei Jing: Children’s Hospital of Chongqing Medical University
Shawn Chen: Tsinghua University
Yun He: Chongqing University

Nature Communications, 2018, vol. 9, issue 1, 1-8

Abstract: Abstract Development of effective antimicrobial agents continues to be a great challenge, particularly due to the increasing resistance of superbugs and frequent hospital breakouts. There is an urgent need for more potent and safer antibiotics with novel scaffolds. As historically many commercial drugs were derived from natural products, discovery of antimicrobial agents from complex natural product structures still holds a great promise. Herein, we report the total synthesis of natural albomycins δ1 (1a), δ2 (1b), and ε (1c), which validates the structures of these peptidylnucleoside compounds and allows for synthetic access to bioactive albomycin analogs. The efficient synthesis of albomycins enables extensive evaluations of these natural products against model bacteria and clinical pathogens. Albomycin δ2 has the potential to be developed into an antibacterial drug to treat Streptococcus pneumoniae and Staphylococcus aureus infections.

Date: 2018
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DOI: 10.1038/s41467-018-05821-1

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