高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 146.

• Organic Synthesis Chemistry • 上一篇    下一篇

Studies on Semisynthesis and Antibacterial Activities of 7β-(l-aryl-5-methyl-l,2,3-triazol-4-acylamido)-3-(2-substituted-1,3,4-oxadizol-5-thiomethyl) Cephalosporin

Xin-Ping HUI1, Peng-Fei XU1, Lan HAO1, Zi-Yi ZHANG1, Zuo-Wu GUAN2   

  1. 1. National Laboratory of Applied Organic Chemistry, Department of Chemistry, Lanzhou University, Lanzhou 730000;
    2. Institute of Applied Pharmacy, Beijing Medical University, Beijing 100083
  • 出版日期:1998-12-31 发布日期:1998-12-31
  • 通讯作者: Peng-Fei XU

Studies on Semisynthesis and Antibacterial Activities of 7β-(l-aryl-5-methyl-l,2,3-triazol-4-acylamido)-3-(2-substituted-1,3,4-oxadizol-5-thiomethyl) Cephalosporin

Xin-Ping HUI1, Peng-Fei XU1, Lan HAO1, Zi-Yi ZHANG1, Zuo-Wu GUAN2   

  1. 1. National Laboratory of Applied Organic Chemistry, Department of Chemistry, Lanzhou University, Lanzhou 730000;
    2. Institute of Applied Pharmacy, Beijing Medical University, Beijing 100083
  • Online:1998-12-31 Published:1998-12-31
  • Contact: Peng-Fei XU

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摘要： Cephalosporin derivatives have been a subject in the field of β-lactam antibiotics due to their broad-spectrum biological activities in recent years. Chemical manipulation of the C-3 and 7β-position in the cephalosporin molecule has resulted in the discovery of numerous novel antibiotics. In general, the C-3 position of the cephalosporin were substituted with heterocyclyl sulfurs or nitrogens and the 7β-position were substituted with heterocycles or aryl1. The side chain at 7β-position determined their antibacterial activities and antibacterial spectrum, moreover, the substituted groups at C-3 position not only affect pharmacokinetic properties, but antibacterial activities and antibacterial spectrum as well.2 Roche Reiner company found that the activities of cephalosporin can be improved by changing the R of RCONH- at 7β-position of 7ACA and introducing various thioazoleheterocycles into C-3 position of it.3 It is no doubt that these heterocycles increased their activities and wided their antibacterial spectrum. In the course of our studies on the modification of cephalosporin, our efforts have been focused on introducing heterocycles into C-3 and 7β-position of 7ACA with the hope of achieving better antibiotics.

Abstract: Cephalosporin derivatives have been a subject in the field of β-lactam antibiotics due to their broad-spectrum biological activities in recent years. Chemical manipulation of the C-3 and 7β-position in the cephalosporin molecule has resulted in the discovery of numerous novel antibiotics. In general, the C-3 position of the cephalosporin were substituted with heterocyclyl sulfurs or nitrogens and the 7β-position were substituted with heterocycles or aryl1. The side chain at 7β-position determined their antibacterial activities and antibacterial spectrum, moreover, the substituted groups at C-3 position not only affect pharmacokinetic properties, but antibacterial activities and antibacterial spectrum as well.2 Roche Reiner company found that the activities of cephalosporin can be improved by changing the R of RCONH- at 7β-position of 7ACA and introducing various thioazoleheterocycles into C-3 position of it.3 It is no doubt that these heterocycles increased their activities and wided their antibacterial spectrum. In the course of our studies on the modification of cephalosporin, our efforts have been focused on introducing heterocycles into C-3 and 7β-position of 7ACA with the hope of achieving better antibiotics.

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