A diversity-oriented rhodamine library for wide-spectrum bactericidal agents with low inducible resistance against resistant pathogens

Xiao Luo, Liujia Qian, Yansheng Xiao, Yao Tang, Yang Zhao, Xia Wang, Luyan Gu, Zuhai Lei, Jianming Bao, Jiahui Wu, Tingting He, Fupin Hu, Jing Zheng, Honglin Li, Weiping Zhu, Lei Shao, Xiaojing Dong, Daijie Chen (), Xuhong Qian () and Youjun Yang ()
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Xiao Luo: East China University of Science and Technology
Liujia Qian: Shanghai Jiao Tong University
Yansheng Xiao: East China University of Science and Technology
Yao Tang: East China University of Science and Technology
Yang Zhao: East China University of Science and Technology
Xia Wang: East China University of Science and Technology
Luyan Gu: East China University of Science and Technology
Zuhai Lei: East China University of Science and Technology
Jianming Bao: Shanghai Institute of Pharmaceutical Industry
Jiahui Wu: Shanghai Institute of Pharmaceutical Industry
Tingting He: East China University of Science and Technology
Fupin Hu: Fudan University
Jing Zheng: East China University of Science and Technology
Honglin Li: East China University of Science and Technology
Weiping Zhu: East China University of Science and Technology
Lei Shao: Shanghai Institute of Pharmaceutical Industry
Xiaojing Dong: Shanghai Institute of Pharmaceutical Industry
Daijie Chen: Shanghai Jiao Tong University
Xuhong Qian: East China University of Science and Technology
Youjun Yang: East China University of Science and Technology

Nature Communications, 2019, vol. 10, issue 1, 1-12

Abstract: Abstract Antimicrobial resistance is a public health emergency and warrants coordinated global efforts. Challenge is that no alternative molecular platform has been identified for discovery of abundant antimicrobial hit compounds. Xanthene libraries have been screened for bioactive compounds. However, the potentially accessible chemistry space of xanthene dyes is limited by the existing xanthene synthesis. Herein we report a mild one-step synthesis, which permits late-stage introduction of a xanthene moiety onto i.e. natural products, pharmaceuticals, and bioactive compounds and construction of a focused library of rhodamine dyes exhibiting facile functional, topographical and stereochemical diversity. In vitro screening yields 37 analogs with mid-to-high bactericidal activity against WHO priority drug-resistant pathogens. These findings suggest that synthetic dye libraries exhibiting high structural diversity is a feasible chemical space combating antibacterial resistance, to complement the natural sources.

Date: 2019
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DOI: 10.1038/s41467-018-08241-3

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