Cephalosporin antibiotics. Synthesis and antimicrobial activity of 7 beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-oxyiminoacetamido]cephalosporin derivatives.
Cephalosporins with a 7 beta-[2-(5-amino-1,2,4-thiadiazol-3-yl) -2-oxyiminoacetamido] side chain were synthesized and their in vitro inhibitory potency was established. The compounds exhibit a strong antibacterial activity against various Gram-positive and Gram-negative bacteria. The antimicrobial activity is related to the oxime-substituent R1 and the C-3 substituent R2. Selected amino-1,2,4-thiadiazolyl-cephems 1 show a prolonged half-life in mice.
D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000378:metabolism / Q000633:toxicity; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006207:Half-Life; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis
D002511:Cephalosporins; D007202:Indicators and Reagents; D013830:Thiadiazoles