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2,5-二取代-1,3,4-噻二唑衍生物的一锅法合成、结构表征及生物活性研究
引用本文:李英俊,孙亚珍,靳焜,许永廷,孙淑琴.2,5-二取代-1,3,4-噻二唑衍生物的一锅法合成、结构表征及生物活性研究[J].有机化学,2008,28(6):1074-1078.
作者姓名:李英俊  孙亚珍  靳焜  许永廷  孙淑琴
作者单位:1. 辽宁师范大学化学化工学院,大连,116029
2. 大连理工大学精细化工国家重点实验室,大连,116012
摘    要:采用超声波辐射与相转移催化联用技术, 一锅法合成出了8个新的2-(1-萘乙酰氨基)-5-芳氨甲基-1,3,4-噻二唑化合物, 这种合成方法具有反应条件温和、反应时间较短、产率较高等特点. 新化合物的结构利用IR, 1H NMR, 13C NMR, 1D NOE, MS和元素分析进行了表征. 人环氧酶-2 (COX-2)活性抑制实验结果表明, 目标化合物5f对COX-2具有很强的抑制活性, 抑制率高达95.59%; 化合物5g对COX-2也具有一定的抑制活性. 目标化合物无抗惊厥活性.

关 键 词:2  5-二取代-1  3  4-噻二唑  一锅法合成  超声波辐射  相转移催化  生物活性
收稿时间:2007-9-22
修稿时间:2007年9月22日

One-Pot Synthesis, Characterization and Biological Activity of 2,5-Disubstituted-1,3,4-thiadiazole Derivatives
LI,Ying-Jun,SUN,Ya-Zhen,JIN,Kun,XU,Yong-Ting,SUN,Shu-Qin.One-Pot Synthesis, Characterization and Biological Activity of 2,5-Disubstituted-1,3,4-thiadiazole Derivatives[J].Chinese Journal of Organic Chemistry,2008,28(6):1074-1078.
Authors:LI  Ying-Jun  SUN  Ya-Zhen  JIN  Kun  XU  Yong-Ting  SUN  Shu-Qin
Institution:( College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029)(State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012)
Abstract:A facile one-pot synthesis of 2,5-disubstituted-1,3,4-thiadiazoles was achieved by ultrasonic irradiation and phase transfer catalysis for the first time and eight novel 2,5-disubstituted-1,3,4-thiadiazoles were synthesized. This method has the advantages of mild conditions, short time, good yields, convenience, economy and environmental friendliness. The structures of the target molecules were characterized by IR, 1H NMR, 13C NMR, 1D NOE, MS spectra and elemental analysis. The experiments of the biological activity for the target molecules were accomplished. The experimental results of the inhibiting activity against COX-2 indicated that the compound 5f had the highest inhibition rate, up to 95.59%, and yet the compound 5g exhibited weakly inhibiting activity. The target compounds did not possess anticonvulasional activity.
Keywords:2  5-disubstituted-1  3  4-thiadiazole  one-pot synthesis  ultrasonic irradiation  phase transfer catalysis  biological activity
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