Synthesis of tetrazole containing 1,2,3-thiadiazole derivatives via U-4CR and their anti-TMV activity |
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| Authors: | Shou-Xin Wang Zhen Fang Zhi-Jin Fan Dun Wang Yue-Dong Li Xiao-Tian Ji Xue-Wen Hua Yun Huang Tatiana A Kalinina Vasiliy A Bakulev Yury Yu Morzherin |
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| Institution: | a School of Basic Sciences, Jining Medical University, Jining 272067, China;
b State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China;
c Department of Plant Pathology, Sichuan Agricultural University, Chengdu 611130, China;
d 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 tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS (ESI). Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL. |
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| Keywords: | 1 2 3-Thiadiazole Tetrazole Anti-TMV activity Ugi reaction |
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