{"title":"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。","authors":"Wei Zeng, Zhiling Sun, Yufang Zhang, Yuzhi Hu, Qing Zhou, Yujiao Qiu, Jieyu Li, Wei Xue","doi":"10.1016/j.fitote.2024.106272","DOIUrl":null,"url":null,"abstract":"<div><div>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 EC<sub>50</sub> values for the curative and protective activity of <strong>S14</strong> against TMV were 91.8 and 130.6 <em>μ</em>g/mL, which was better than that of the antiviral agent ningnanmycin (NNM, 237.8, 220.6 <em>μ</em>g/mL). The results of preliminary mechanism study indicated that <strong>S14</strong> 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 <strong>S14,</strong> so that it can enhance the photosynthetic capacity of plants. In addition, the results of malondialdehyde (MDA) content assay also indicated that <strong>S14</strong> could improve the disease resistance of tobacco.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"179 ","pages":"Article 106272"},"PeriodicalIF":2.5000,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"New chalcone derivatives containing morpholine-thiadiazole: Design, synthesis and evaluation of against tobacco mosaic virus\",\"authors\":\"Wei Zeng, Zhiling Sun, Yufang Zhang, Yuzhi Hu, Qing Zhou, Yujiao Qiu, Jieyu Li, Wei Xue\",\"doi\":\"10.1016/j.fitote.2024.106272\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>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 EC<sub>50</sub> values for the curative and protective activity of <strong>S14</strong> against TMV were 91.8 and 130.6 <em>μ</em>g/mL, which was better than that of the antiviral agent ningnanmycin (NNM, 237.8, 220.6 <em>μ</em>g/mL). The results of preliminary mechanism study indicated that <strong>S14</strong> 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 <strong>S14,</strong> so that it can enhance the photosynthetic capacity of plants. In addition, the results of malondialdehyde (MDA) content assay also indicated that <strong>S14</strong> could improve the disease resistance of tobacco.</div></div>\",\"PeriodicalId\":12147,\"journal\":{\"name\":\"Fitoterapia\",\"volume\":\"179 \",\"pages\":\"Article 106272\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-10-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Fitoterapia\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0367326X24004556\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fitoterapia","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0367326X24004556","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
New chalcone derivatives containing morpholine-thiadiazole: Design, synthesis and evaluation of against tobacco mosaic virus
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.
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.
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