Synthesis and antibacterial activity of C-7 haloacyl cephalosporins
10.16438/j.0513-4870.2021-0337
- VernacularTitle:C-7位卤代酰基头孢化合物的合成及其抗菌活性研究
- Author:
Yang LI
1
;
Li FAN
1
;
Xue-mei TANG
2
;
De-meng YANG
1
;
Jun-hua HU
3
;
Yu-zhu WU
3
;
Shuang ZHAN
3
;
Da-cheng YANG
1
Author Information
1. Key Laboratory of Applied Chemistry of Chongqing Municipality, Institute of Bioorganic and Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
2. Science and Technology Division, Southwest University, Chongqing 400715, China
3. Citrus Research Institute, Southwest University, Chongqing 400715, China
- Publication Type:Research Article
- Keywords:
cephalosporin;
halogenated acid chloride;
activity against human pathogenic bacteria;
activity against pichia pastoris;
anti-citrus canker activity;
activity against citrus pathogenic fungi
- From:
Acta Pharmaceutica Sinica
2021;56(7):1965-1975
- CountryChina
- Language:Chinese
-
Abstract:
Cephalosporins are widely used in the treatment of infectious diseases. The structural differences in cephalosporin drugs mainly lie in the C-7 amino side chain and the C-3 substituent. In this study, twenty-five haloacylated cephalosporins of five series were designed by using a strategy of introducing simple substituents at the C-7 amino group in four cephalosporin parent nucleus with different C-3 substituents and efficiently synthesized under optimized conditions. Their activities against human pathogenic bacteria, Pichia pastoris, citrus canker and citrus pathogenic fungi were evaluated. The results showed that most of the molecules had activity against human pathogenic bacteria, of which seven compounds including TM1f had stronger or equivalent inhibitory activities against eight human pathogens than the marketed drugs cefalotin, cefoxitin sodium and ceftizoxime sodium. The inhibitory activity of TM1s against Alternaria alternate Al.6 was stronger than that of cephalosporins and comparable to that of the positive control prochloraz. TM1f and TM1s are worthy of further study.
