Synthesis and antiviral evaluation of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates |
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Authors: | Xiuhai Gan Deyu Hu Zhuo Chen Yanjiao Wang Baoan Song |
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Institution: | 1. State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research, and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025, China;2. College of Chemistry and Life Science, Guizhou Education University, Guiyang 550018, China |
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Abstract: | A series of novel 1,3,4-oxadiazole/thiadiazole–chalcone conjugates were synthesized and their in vitro and in vivo antiviral activities were evaluated via microscale thermophoresis method and half-leaf method, respectively. The in vitro results indicated that compounds 7g, 7l, 8h, and 8l displayed good antiviral activity against TMV, with the binding constant values of 5.93, 6.15, 6.02, and 5.04 μM, respectively, which were comparable to that of Ninnanmycin (6.78 μM) and even better than that of Ribavirin (99.25 μM). The in vivo results demonstrated that compounds 7g, 7l, 8h, and 8l exhibited remarkable anti-TMV activity with the EC50 values of 33.66, 33.97, 33.87 and 30.57 µg/mL, respectively, which were comparable to that of Ningnanmycin (36.85 µg/mL) and superior to that of Ribavirin (88.52 µg/mL). Interestingly, the trend of antiviral activity in vivo was consistent with the in vitro results. |
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Keywords: | TMV tobacco mosaic virus HRMS high-resolution mass spectrometer half-maximal effective concentration MST microscale thermophoresis SAR structure–activity relationship TMV CP tobacco mosaic virus coat protein Chalcone 1 3 4-Oxadiazole/thiadiazole Tobacco mosaic virus coat protein Antiviral activity Microscale thermophoresis |
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