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Studies on 3'-quaternary ammonium cephalosporins--IV. Synthesis and antibacterial activity of 3'-(2-alkyl-3-aminopyrazolium) cephalosporins related to FK037.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 1997 Aug; Vol. 5 (8), pp. 1685-94. - Publication Year :
- 1997
-
Abstract
- The synthesis and in vitro antibacterial activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido] cephalosporins bearing various 2-alkyl-3-aminopyrazolium groups at the 3-position are described. Antibacterial activity against MRSA was affected by the nature of the substituent at the 2-position on the 3'-aminopyrazolium groups. Among the cephalosporins prepared in this study, 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[3-am ino-2-(2 -hydroxyethyl)-pyrazolio]methyl-3-cephem-4-carboxylate sulfate (23e, FK037) showed extremely potent broad-spectrum activity against both Gram-positive bacteria including MRSA, and Gram-negative bacteria including Pseudomonas aeruginosa. In particular, the in vivo activity against MRSA of FK037 was the highest of all the beta-lactam antibiotics tested.
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents pharmacology
Ceftizoxime chemistry
Ceftizoxime pharmacology
Cephalosporins chemistry
Cephalosporins pharmacology
Microbial Sensitivity Tests
Models, Molecular
Ceftizoxime analogs & derivatives
Cephalosporins chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 5
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 9313870
- Full Text :
- https://doi.org/10.1016/s0968-0896(97)00092-8