Synthesis of 3,5-Dichloro-4-(1,1,2,2-tetrafluoroethoxy)phenyl Containing 1,2,3-Thiadiazole Derivatives via Ugi Reaction and Their Biological Activities |
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| Authors: | Wang Shouxin Wang Huan Fan Zhijin Fu Yifeng Mi Na Zhang Jufang Zhang Zhengcai Belskaya Nataliya P Bakulev Vasiliy A |
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| Institution: | 1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China;2. State Key Laboratory of Elemento Organic Chemistry, Nankai University, Tianjin 300071, China;3. The Ural Federal University Named After the First President of Russia B. N. Yeltsin, Yeltsin UrFU, 620002, Ekaterinburg, Russia |
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| Abstract: | A series of novel 3,5‐dichloro‐4‐(1,1,2,2‐tetrafluoroethoxy)phenyl containing 4‐methyl‐1,2,3‐thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by IR, 1H NMR, 13C NMR and high‐resolution mass spectroscopy. The preliminary bioassay results indicated that some title compounds had good fungicide activity at 50 µg/mL; most of the compounds presented a certain degree of direct inhibition activity, good inactivation and curative activity against tobacco mosaic virus at 500 µg/mL and 100 µg/mL; some compounds showed good larvicidal activity against Plutella xylostella L. at 200 µg/mL and excellent larvicidal activities against Culex pipiens pallens at 2 µg/mL. |
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| Keywords: | 1 2 3‐thiadiazole Ugi reaction synthesis design biological activity multicomponent reactions |
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