New cephalosporins with 7-acyl groups derived from .BETA.-ketoacids. II. Further modifications of 7-(3-oxobutyrylamino)-cephalosporins.
- 1 January 1978
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 31 (12) , 1252-1261
- https://doi.org/10.7164/antibiotics.31.1252
Abstract
New cephalosporins modified in the acyl part of 7-(3''-oxobutyrylamino)cephalosporins (1) were synthesized by thiolation at the 2''- or the 4''-position, or by transforming the 3''-oxo group into a 3''-imino group. The most active compound in vitro was 3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-7-(4-methylthio-3-oxobutyrylamino)ceph-3-em-4-carboxylic acid (7c), which showed superior in vitro activity against gram-positive and gram-negative bacteria compared to the parent cephalosporin (1b) with the same 3-substituent. The ED50 value for 7c was essentially equal to that of 1b in mice infected with Escherichia coli O-111.This publication has 1 reference indexed in Scilit:
- New cephalosporins with 7-acyl groups derived from .BETA.-ketoacids. I. 7-(.BETA.-Ketoacylamino)cephalosporins.The Journal of Antibiotics, 1978