126352-82-7Relevant academic research and scientific papers
Studies on 3'-quaternary ammonium cephalosporins - III. Synthesis and antibacterial activity of 3'-(3-aminopyrazolium)cephalosporins
Ohki, Hidenori,Kawabata, Kohji,Inamoto, Yoshiko,Okuda, Shinya,Kamimura, Toshiaki,Sakane, Kazuo
, p. 557 - 567 (2007/10/03)
The synthesis and in vitro antibacterial activity of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido] cephalosporins bearing N-mono or dialkyl and carbamoyl aminopyrazolium, and five- or six-membered rings fused to the 3-aminopyrazolium methyl groups at the 3-position, are described. Aminopyrazolium methyl cephalosporins (23e, f, i), with fused saturated and unsaturated rings were especially effective against Staphylococcus strains compared to 3-amino-2-methylpyrazolium methyl cephalosporin (1). Among the cephalosporins prepared in this work, 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyimino acetamidol-3-(4,5,6,7-tetrahydro-1-pyrazolo[1,5-a] pyrimidinio)methyl-3-cephem-4-carboxylate (23f) showed a good balance of antibacterial activity against both Gram-positive bacteria including Staphylococcus aureus and Gram-negative bacteria including P. aeruginosa. An imidazopyrazolium group at the 3-position in, for example, cephalosporin (23i) was particularly effective for improving antibacterial activity against MRSA.
Cephem compounds
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, (2008/06/13)
The invention relates to an antimicrobial compound of the formula: STR1 wherein R1 is amino or a protected amino group, R2 is lower alkyl, lower alkenyl, carboxy (lower) alkyl or protected carboxy(lower)alkyl, R3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl, protected amino(lower)alkyl or lower alkanoyl, R4 is hydrogen, lower alkyl or lower alkylthio, and Z is N or CH or a pharmaceutically acceptable salt thereof.
