Synthesis and biological activity of 7 beta-(2-amino-2-carboxy)-ethylthioacetamido-7 alpha-methoxycephalosporin derivatives.
C-7 and C-3 substituents of a new antibiotic SF-1623 were chemically modified to improve the bioactivity, and substituent effect at C-7 and C-3 was examined on the basis of MIC and ED50 values against selected bacteria. Among a large number of derivatives, MT-141 possessing 2-D-2-amino-2-carboxyethylthioacetamido residue at C-7 and N-methyltetrazolyl-thiomethyl residue at C-3 showed a high order of antibacterial activity in vitro and especially in vivo.
D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds
D002511:Cephalosporins; D013438:Sulfhydryl Compounds