144991-33-3Relevant academic research and scientific papers
Studies on 3'-quaternary ammonium cephalosporins-IV. Synthesis and antibacterial activity of 3'-(2-alkyl-3-aminopyrazolium)cephalosporins related to FK037
Ohki, Hidenori,Kawabata, Kohji,Inamoto, Yoshiko,Okuda, Shinya,Kamimura, Toshiaki,Sakane, Kazuo
, p. 1685 - 1694 (2007/10/03)
The synthesis and in vitro antibacterial activity of 7β-[(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, 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[3-amino-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 β-lactam antibiotics tested.
