Synthesis of baicalein derivatives and evaluation of their antiviral activity against arboviruses

Bioorg Med Chem Lett. 2022 Sep 15:72:128863. doi: 10.1016/j.bmcl.2022.128863.

Xi-Jing Qian ¹, He-Yang Zhou ², Yan Liu ¹, Jia-Xiao Dong ², Wan-Da Tang ¹, Ping Zhao ¹, Hai-Lin Tang ³, Yong-Sheng Jin ⁴

Affiliations

1 Department of Microbiology, Faculty of Naval Medicine, Naval Medical University, Shanghai 200433, China.
2 Department of Organic Chemistry, School of Pharmacy, Naval Medical University, Shanghai 200433, China.
3 Department of Microbiology, Faculty of Naval Medicine, Naval Medical University, Shanghai 200433, China. Electronic address: hailint@163.com.
4 Department of Organic Chemistry, School of Pharmacy, Naval Medical University, Shanghai 200433, China. Electronic address: ysjin@smmu.edu.cn.

PMID: 35738350 DOI: 10.1016/j.bmcl.2022.128863

Abstract

Natural plant-derived baicalein which is extracted from Chinese herb Scutellaria baicalensis Georgi belongs to the flavonoid compounds and possesses multiple pharmacological activities. In this study, we designed and synthesized new series of derivatives of baicalein (BE) through catalytic coupling reactions, and screened for their Antiviral activity against arboviruses including Chikungunya virus (CHIKV), West Nile virus (WNV) or Zika virus (ZIKV). Our results revealed for the first time that BE and its derivatives had potent anti-CHIKV, anti-WNV and anti-ZIKV effects. And modification of 8 or 4' position could lead to obtain potent Antiviral compounds against CHIKV, WNV and ZIKV with lower cytotoxicity. Among the baicalein derivatives, C3 and F3 showed the most potent Antiviral activities against CHIKV, WNV and ZIKV, which were 5-10 times more potent than baicalein. Our findings will provide research basis for the development of baicalein derivatives as effective Antiviral agents.

Keywords

Baicalein; Chikungunya virus; Synthesis; West Nile virus; Zika virus.

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