Design,Synthesis, and Antifungal Activities of Novel Carboxamides Derivatives Bearing a Chalcone Scaffold as Potential SDHIs |
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Authors: | Bo Luo Chongchong Zhang Suya Liang Wei Zhou Yihan Hu Yulin Li Jiayi Hu Lailiang Qu |
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Institution: | 1. College of Life Sciences, Xinyang Normal University, Tea Plant Biology Key Laboratory of Henan Province, Xinyang, 464000 China;2. College of Medicine, Xinyang Normal University, Xinyang, 464000 China |
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Abstract: | In search for SDHIs fungicides, twenty-five novel carboxamides containing a chalcone scaffold were designed, synthesized, and evaluated for antifungal activities against five pathogenic fungi. The results showed that compound 5 k exhibited outstanding antifungal activity against R. solani with an EC50 value of 0.20 μg/mL, which was much better than that of commercial SDHIs Boscalid (EC50=0.74 μg/mL). Moreover, compound 5 k also displayed promising antifungal activities against S. sclerotiorum, B. cinerea, and A. alternate (IC50=2.53–4.06 μg/mL), indicating that 5 k had broad-spectrum antifungal activity. Additionally, in vivo antifungal activities results showed that 5 k could significantly inhibit the growth of R. solani in rice leaves with good protective efficacy (57.78 %) and curative efficacy (58.45 %) at 100 μg/mL, both of which were much better than those of Boscalid, indicating a promising application prospect. Moreover, SEM analysis showed that compound 5 k could remarkably disrupt the typical structure and morphology of R. solani hyphae. Further SDH enzyme inhibition assay and molecular docking study revealed that lead compound 5 k had a similar mechanism of action as commercial SDHI Boscalid. These results indicated that compound 5 k showed potential as a SDHIs fungicide and deserved further investigation. |
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Keywords: | antifungal activities carboxamides chalcone scaffold mechanism of action SDHIs |
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