Synthesis of tetrazole containing 1,2,3-thiadiazole derivatives via U-4CR and their anti-TMV activity  

作　　者：Shou-Xin Wanga 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 

机构地区：[1]School of Basic Sciences,Jining Medical University [2]State Key Laboratory of Elemento-Organic Chemistry,Nankai University [3]Department of Plant Pathology,Sichuan Agricultural University [4]The Ural Federal University Named after the First President of Russia B.N.Yeltsin

出　　处：《Chinese Chemical Letters》2013年第10期889-892,共4页中国化学快报（英文版）

基　　金：funded in part by the NSF of Tianjin (No. 10JCZDJC17500);the National Key Project for Basic Research (No. 2010CB126105);National Key Technology Research and Development Program (No. 2011BAE06B02);the Foundation of Achievements Transformation and Application of Tianjin Agricultural Science and Technology (No. 201002250);Tianjin Key Technology Research and Development Program (No. 11ZCGYNC00100);The Commonweal Specialized Research Fund of China Agriculture (Nos. nyhyzx3-21, 201103016 and 201003029)

摘　　要：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.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.

关 键 词：1 2 3-Thiadiazole Tetrazole Anti-TMV activity Ugi reaction 

分 类 号：O626.12[理学—有机化学]