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《中国化学快报(英文版)》 2015-10
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Synthesis and biological activities of novel 2-amino-1,3-thiazole-4-carboxylic acid derivatives

Feng-Yun Li;Xiao-Feng Guo;Zhi-Jin Fan;Yu-Qing Zhang;Guang-Ning Zong;Xiao-Lin Qian;Liu-Yong Ma;Lai Chen;Yu-Jie Zhu;Kalinina Tatiana;Yury Yu.Morzherin;Nataliya P.Belskaya;State Key Laboratory of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering, Nankai University;The Ural Federal University Named after the First President of Russia B.N.Yeltsin;  
A series of novel 2-amino-1,3-thiazole-4-carboxylic acid derivatives were designed and synthesized.Their structures were confirmed by melting points, IR,1H NMR,13 C NMR, and HRMS or elemental analysis. Biological activities of all title compounds including fungicidal activity and antivirus activity were evaluated systematically. Preliminary bioassays indicated that these compounds exhibited good fungicidal activity at 50 mg/m L, compounds 4b and 4i exhibited over 50% activity against six fungi tested.Most compounds showed good activity against TMV with different models in vivo at 100 mg/m L.Compounds 4c and 4e stood out with high effects against TMV in vivo in all models tested, including protective, inactivative, curative, and inductive activities. These data demonstrate a new strategy for fungi and virus control.
【Fund】: supported by The International Science & Technology Cooperation Program of China (No.2014DFR41030);; Nataliya P. Belskaya thanks Russian State Task of Ministry Education and Science (No.4.560.2014/K );; Kalinina Tatiana thanks RFBF (No.13-03-00137)
【CateGory Index】: O626.25
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