The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF A NEW SERIES OF CEPHALOSPORINS, El040 AND RELATED COMPOUNDS
ISAO SUGIYAMAYUUKI KOMATSUHIROSHI YAMAUCHI
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1992 Volume 45 Issue 1 Pages 103-112

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Abstract

The synthesis and in vitro antibacterial activity of a series of 7-[(Z)-2-aminoaryl-2-oxyiminoacetamido]-3-ammoniomethyl-3-cephems are described. Variation of an oxyimino moiety with aminoaryl at the C-7 side chain and a quaternary ammonium moiety at the C-3 side chain were examined and structure-activity relationships were studied.
E1040, the 3-(4-carbamoylquinuclidinio)methyl derivative of the 7-α-methoxyimino series of aminothiadiazolyl cephalosporins, exhibited excellent activity against both Gram-positive and Gram-negative bacteria, particularly against Pseudomonas aeruginosa, and possessed high stability to β-lacctamases.

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