Synthesis and antibacterial activity of 7 beta-2-(2-substituted aminothiazol-4-yl)-(Z)-2-methoxyiminoacetylamido-3-quaternaryammoniummethyl-cephalosporins.
- Author:
Guo-hua CHEN
1
;
Yang YANG
;
Zhong REN
;
Qi-xing ZHONG
Author Information
1. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Anti-Bacterial Agents;
chemical synthesis;
chemistry;
pharmacology;
Cephalosporins;
chemical synthesis;
chemistry;
pharmacology;
Gram-Negative Bacteria;
drug effects;
Gram-Positive Bacteria;
drug effects;
Molecular Structure;
Staphylococcus aureus;
drug effects;
Streptomyces;
drug effects
- From:
Acta Pharmaceutica Sinica
2009;44(4):366-370
- CountryChina
- Language:Chinese
-
Abstract:
In order to find new cephalosporin with more and more potent antibacterial activity, nine new fourth-generation cephalosporins (N1-N9) were synthesized from ethyl 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetate (1) via acylation, substitution, hydrolysis, active esterification, condensation and salt formation. The structures of compounds (N1-N9) were confirmed by IR, MS, 1H NMR and elemental analysis. The target compounds possess different antimicrobial activities against Gram-positive and Gram-negative bacteria. The preliminary results of antibacterial activities revealed that they showed better antibacterial activities against Gram-positive bacteria than cefpirome sulfate. In particular, their activities against Staphylococcus aureus and Streptococcus albus are better.
