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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Ohki H,Kawabata K,Inamoto Y,Okuda S,Kamimura T,Sakane Kdoi
10.1016/s0968-0896(97)00092-8subject
Has Abstractpub_date
1997-08-01 00:00:00pages
1685-94issue
8eissn
0968-0896issn
1464-3391pii
S0968089697000928journal_volume
5pub_type
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