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Published on: May 10, 2022
Development of bivalent oleanane-type triterpenes as potent HCV entry inhibitors
Fei Yu1, Yiyun Peng2, Qi Wang3
1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China; Medical Faculty of Kunming University of Science and Technology, Kunming 650500, China.
Abstract:
The development of entry inhibitors is an emerging approach to the prevention and reduction of HCV infection. Starting from echinocystic acid (EA), a μM HCV entry inhibitor, we have developed a series of bivalent oleanane-type triterpenes which, upon optimization of the length, rigidity and hydrophobicity of the linker, exert dramatically potent enhancement of inhibition with IC50 values extending into the nM level. This study establishes the importance of triterpene natural products as new leads in the development of potential HCV entry inhibitors.
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