Studies on monocyclic .BETA.-lactam antibiotics. II. Synthesis and antibacterial activity of 3-acylamino-2-azetidinone-1-oxysulfonic acids.
- 1 January 1985
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 38 (11) , 1536-1549
- https://doi.org/10.7164/antibiotics.38.1536
Abstract
The synthesis and in vitro antibacterial and .beta.-lactamase inhibitory activity of the 2-azetidinone-1-oxysulfonic acids having a substituent at C-4 position of the .beta.-lactam ring are described. The influence of C-4 substituents on the antibacterial activity was examined for the compounds having .alpha.-ureidoacetyl or .alpha.-oxyiminoacetyl group as acyl side chain at C-3 position. The antibacterial activity is correlated with the C-4 substituents and acyl side chain. Especially, 4(R)-methyl substituted derivatives exhibited excellent activity against Gram-negative bacteria and 4-dimethyl substituted derivatives exhibited strong activity against resistant Gram-negative bacteria except for Pseudomonas aeruginosa. 39 and 40 showed strong inhibitory activity against cephalosporinase of Enterobacter cloacae H-27.This publication has 13 references indexed in Scilit:
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