- Studies on 3'-quaternary ammonium cephalosporins-IV. Synthesis and antibacterial activity of 3'-(2-alkyl-3-aminopyrazolium)cephalosporins related to FK037
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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.
- Ohki, Hidenori,Kawabata, Kohji,Inamoto, Yoshiko,Okuda, Shinya,Kamimura, Toshiaki,Sakane, Kazuo
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- Cephem compound
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The invention relates to antimicrobial compounds of the formula: STR1 wherein R1 is amino or a protected amino, R2 is ethyl, propyl or lower alkenyl, R3 is COO θ, carboxy or a protected carboxy, R4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R5 is amino or a protected amino, Xθ is an anion, and n is 0 or 1, or, R1, R3, R5, Xθ and n are each as defined above, R2 is lower alkyl, and R4 is 3-hydroxypropyl, with proviso that (i) when R3 is COOθ, then n is 0, and (ii) when R3 is carboxy or a protected carboxy, then n is 1, or a pharmaceutically acceptable salt thereof.
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- Cephem compounds and processes for preparation thereof
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7 β-[2-5 amino-1, 2, 4 thiadiazol-3yl) 2(carboxy lower alkyleneoxyimino) acetamido]-3-(3-amino-2-alkyl-1-pyrazolio) methyl 3 cephem 4 carboxylates are prepared. They are antibiotics.
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- Cephem compound and a process for preparation thereof
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The object of the invention is a new cephem compound with antimicrobial activity used for the treatment of infectious diseases of the general formula: STR1 wherein R1 is amino or a protected amino R2 is lower alkyl which may have 1 to 3 halogens R3 is COO?, carboxy or a protected carboxy R4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl R5 is amino or a protected amino R6 is hydrogen or lower alkyl X? is an anion, and n is 0 or 1 with proviso that (i) when R3 is COO?, then n is 0, and (ii) when R3 is carboxy or a protected carboxy, then n is 1, and pharmaceutically acceptable salt thereof.
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