New chalcone derivatives containing morpholine-thiadiazole: Design, synthesis and evaluation of against tobacco mosaic virus

IF 2.5 3区医学 Q3 CHEMISTRY, MEDICINAL

Fitoterapia Pub Date : 2024-10-22 DOI:10.1016/j.fitote.2024.106272

Wei Zeng, Zhiling Sun, Yufang Zhang, Yuzhi Hu, Qing Zhou, Yujiao Qiu, Jieyu Li, Wei Xue

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Abstract

Twenty chalcone derivatives containing morpholine-thiadiazole were designed and synthesized from the natural product chalcone. The bioactivity test results indicate that some compounds exhibit good antiviral activity against tobacco mosaic virus (TMV). In particular, the EC₅₀ values for the curative and protective activity of S14 against TMV were 91.8 and 130.6 μg/mL, which was better than that of the antiviral agent ningnanmycin (NNM, 237.8, 220.6 μg/mL). The results of preliminary mechanism study indicated that S14 had strong binding capacity and affinity to tobacco mosaic virus coat protein (TMV-CP). In the chlorophyll content assay, the chlorophyll content of tobacco leaves increased significantly after the action of S14, so that it can enhance the photosynthetic capacity of plants. In addition, the results of malondialdehyde (MDA) content assay also indicated that S14 could improve the disease resistance of tobacco.

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含有吗啉-噻二唑的新查尔酮衍生物：针对烟草花叶病毒的设计、合成和评估。

从天然产物查尔酮中设计并合成了 20 个含有吗啉-噻二唑的查尔酮衍生物。生物活性测试结果表明，一些化合物对烟草花叶病毒（TMV）具有良好的抗病毒活性。其中，S14 对 TMV 的治疗活性和保护活性的 EC50 值分别为 91.8 和 130.6 μg/mL，优于抗病毒药物宁南霉素（NNM，237.8、220.6 μg/mL）。初步机理研究结果表明，S14 与烟草花叶病毒衣壳蛋白（TMV-CP）具有很强的结合能力和亲和力。在叶绿素含量测定中，S14 作用后烟草叶片的叶绿素含量显著增加，因此它能增强植物的光合能力。此外，丙二醛（MDA）含量测定结果也表明，S14 能提高烟草的抗病性。

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来源期刊

Fitoterapia 医学-药学

CiteScore

5.80

自引率

2.90%

发文量

198

审稿时长

1.5 months

期刊介绍： Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.