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
- ISSN号:1001-604X
- 期刊名称:《中国化学:英文版》
- 时间:0
- 分类:O623.5[理学—有机化学;理学—化学] TG174.42[金属学及工艺—金属表面处理;金属学及工艺—金属学]
- 作者机构:[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 NamedAfier the First President of Russia B. N. Yeltsin, Yeltsin UrFU, 620002, Ekaterinburg, Russia
- 相关基金:Project supported by the National Natural Science Foundation of China (Nos. 20872071, 20911120069), the Tianjin Natural Science Foundation (No. 10JCZDJC17500), the National Key Project for Basic Research (No. 2010CB126105), the National Key Technology Research and Development Program (Nos. 2011BAE06B02, 2011BAE06B05) and the Foundation of Achievements Transformation and Spreading of Tianjin Agricultural Science and Technology (No. 201002250), the Russian Foundation for Basic Research (Nos. RFBR 08-03-00376 a and RFBR/NNSF 08-03-92208 a).
关键词:
噻二唑衍生物, Ugi反应, 生物活性, 反应合成, 苯基, 四氟, 标题化合物, 烟草花叶病毒, 1,2,3-thiadiazole, Ugi reaction, synthesis design, biological activity, multicomponent reactions
中文摘要:
包含 4-methyl-1,2,3-thiadiazole 衍生物的一系列新奇 3,5-dichloro-4-(1,1,2,2-tetrafluoroethoxy ) 苯基经由 Ugi 反应被设计并且综合。他们的结构被红外, 1H NMR, 13C NMR 和高分辨率的集体光谱学证实。初步的生物鉴定结果显示一些标题混合物在 50 g/mL 举办了好杀真菌剂活动;大多数混合物在 500 g/mL 和 100 g/mL 对烟草马赛克病毒介绍了直接抑制活动,好 inactivation 和药品活动的某个度;一些混合物对 Plutella xylostella L 显示出好 larvicidal 活动。在对在 2 g/mL 的一种蚊虫 pipiens pallens 的 200 g/mL 和优秀 larvicidal 活动。
英文摘要:
A series of novel 3,5-dichloro-4-(1,1,2,2-tetrafluoroethoxy)phenyl containing 4-methyl-l,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 ug/mL; most of the compounds presented a certain degree of direct inhibition activity, good inactivation and curative activity against tobacco mosaic virus at 500 ug/mL and 100 ug/mL; some compounds showed good larvicidal activity against Plutella xylostella L. at 200 ug/mL and excellent larvicidal activities against Culex pipiens pallens at 2 ug/mL.