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Synthesis and biological evaluation of fluorinated bergenin derivatives
Hui Zhang1, Ya-Li Xu1, Lin Dong1
1Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, China. dongl@scu.edu.cn.
Abstract:
Bergenin is a natural C-glycoside with multi-target therapeutic potential. Herein, a series of 21 novel derivatives were designed and synthesized through direct hydroxy-fluorination and the incorporation of fluorinated building blocks. Biological activity evaluation results demonstrated that, except for ether derivatives, most fluorine-containing derivatives exhibited superior anti-inflammatory and antitussive activities compared with bergenin, and among these derivatives, the C4-fluorinated ones (1b, 1d, 2a, 2d and 2e) showed the most prominent activity.
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