Chin. J. Org. Chem. ›› 2006, Vol. 26 ›› Issue (12): 1704-1708. Previous Articles     Next Articles




  1. (a兰州大学化学化工学院 功能有机分子化学国家重点实验室 兰州 730000)
    (b兰州大学生命科学学院 兰州 730000)
    (c北京大学医学部 北京 100083)
  • 收稿日期:2006-01-13 修回日期:2006-03-13 发布日期:2006-11-21
  • 通讯作者: 张自义

Semisynthesis and Antibacterial Activity of 7β-[2-(2-Aminothiazol-4- yl)-(Z)-2-methoxyiminoacetylamido]-3-heterothiomethyl-cephalosporins

HUI Xin-Ping*,a,WANG Qinb,WANG Fangb,ZHANG Zi-Yi*,a,GUAN Zuo-Wuc   

  1. (a State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering,
    Lanzhou University
    , Lanzhou 730000)
    (b School of Life Sci-ences, Lanzhou University, Lanzhou 730000)
    (c Peking University Health Science Center, Beijing 100083)
  • Received:2006-01-13 Revised:2006-03-13 Published:2006-11-21
  • Contact: ZHANG Zi-Yi

New cephalosporin derivatives 5a5j were prepared by condensation of 3a~3j with aminothiazoleoxime active ester 4. The intermediates 3a3j were synthesized by the reaction of 5-substituted-1,3,4- oxadiazole-2-thiols (2a2h), 5-arylamino-1,3,4-thiadiazole-2-thiols (2i2j) with 7-aminocephalosporanic acid (7-ACA), respectively. The preliminary results of antibacterial activities revealed that compounds 5 showed obviously antibacterial activities against both Gram-positive and Gram-negative bacteria.

Key words: centrifugal-TLC, semisynthesis, antibacterial activity, cephalosporin