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Synthesis of novel naphthalene-chimonanthine scaffolds hybrids with potent antibacterial or antifungal activity

Shaojun ZhengSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, China.;WU Wen-binSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, China.;Qiaoju JiangSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, China.;Chuansong LinYue FangHuihui DaiBing TangSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, China.;Yi TanSchool of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang, Jiangsu, China.;
2022en
ABI

Abstract

In this work, a total of 19 novel naphthalene hybrids with chimonanthine scaffolds were efficiently synthesised from indole-3-acetonitrile in good yields. The prepared compounds were evaluated for biological activity against Cryptococcus neoformans, Escherichia coli, Shigella spp, Candida albicans, Salmonella spp, and Staphylococcus aureus. The preliminary bioassays showed that most of the synthesised compounds exhibited significant antibacterial or antifungal activity. Notably, compound 8 showed potent activity against Cryptococcus neofonmans, Escherichia coli, Shigella spp, and Candida albicans than the positive control, all with the same MIC value of 3.53 µM. Compound 8 had a broad spectrum of antibacterial or antifungal activity, and will be studied further.

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