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. 2025 Apr;29(2):1091-1107.
doi: 10.1007/s11030-024-10894-w. Epub 2024 Jul 24.

Design, synthesis and antiviral activity of indole derivatives containing quinoline moiety

Bangcan He  1 , Yuzhi Hu  1 , Yishan Qin  1 , Yufang Zhang  1 , Xingping Luo  1 , Zhenchao Wang  2 , Wei Xue  3
Affiliations

Design, synthesis and antiviral activity of indole derivatives containing quinoline moiety

Bangcan He et al. Mol Divers. 2025 Apr.

Abstract

A series of indole derivatives containing quinoline structures were designed and synthesized. The synthesized compounds were characterized by NMR and HRMS. And W14 was performed by single crystal X-ray diffraction experiments. The antiviral activity studies showed that some of the target compounds possessed significant activity against tobacco mosaic virus (TMV). In particular, W20 had significant activity. The results of in vivo anti-TMV activity assay showed that W20 possessed the best curative and protective activities with EC50 values of 84.4 and 65.7 μg/mL, which were better than ningnanmycin (NNM) 205.1 and 162.0 μg/mL, respectively. The results of Microscale thermophoresis (MST) showed that W20 had a strong binding affinity for the tobacco mosaic virus coat protein (TMV-CP) with a dissociation constant (Kd) of 0.00519 μmol/L, which was superior to that of NNM (1. 65320 μmol/L). The molecular docking studies were in accordance with the experimental results. In addition, the determination of malondialdehyde (MDA) content in tobacco leaves showed that W20 improved the disease resistance of tobacco. Overall, this study shows that indole derivatives containing quinoline can be used as new antiviral agents for plant viruses for further research.

Keywords: Antiviral activity; Indole; Quinolone; Tobacco mosaic virus.

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Conflict of interest statement

Declarations. Conflict of interest: The authors declare that there are no competing financial interests.

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