Acta Chimica Sinica ›› 2007, Vol. 65 ›› Issue (9): 834-840. Previous Articles     Next Articles

Original Articles

酰基硫脲衍生物的合成、结构表征及生物活性研究

李英俊*,1, 张治广1, 靳焜2, 彭勤纪2, 丁万刚1, 刘军1   

  1. (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)
  • 投稿日期:2006-08-28 修回日期:2006-11-20 发布日期:2007-05-14
  • 通讯作者: 李英俊

Synthesis, Characterization and Biological Activities of Acylthiourea Derivatives

LI Ying-Jun*,1; ZHANG Zhi-Guang1; JIN Kun2; PENG Qin-Ji2; DING Wan-Gang1; LIU Jun1   

  1. (1 College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029)
    (2 State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012)
  • Received:2006-08-28 Revised:2006-11-20 Published:2007-05-14
  • Contact: LI Ying-Jun

Fifteen new diacyl thioureas with asymmetric structure (compounds 6 and 6') and nine new monoacyl thioureas containing amido group in molecules (compounds 7 and 7') were synthesized by the techniques of ultrasonic irradiation and phase transfer catalysis for the first time. Their structures were confirmed by IR, 1H NMR, 13C NMR, APT, 1D NOE, 2D NMR and elemental analysis. The downfield proton and carbon signals in 1H NMR and 13C NMR spectra have been assigned. The results of screening tests for bactericidal activity, insecticidal activity and herbicidal activity indicated that the target compounds possessed relatively high inhibiting activity against Cl-colletotrichum lagenariun and the compound 6e had the highest inhibition rate, up to 62.4%. The target compound 7a exhibits inhibiting activity against Sf-sphaerotheca fuliginea. Monoamine oxidase activity test showed that most of the target compounds possessed inhibiting activity against monoamine oxidase and the compounds 6'c and 6'd displayed quite higher inhibiting activity than the others at the concentration of 1×10-3 molL-1. The target compounds did not possess anticonvulasional activity.

Key words: acylthiourea, synthesis, ultrasonic irradiation and phase transfer catalysis, biological activity