Laboratory evaluation of BL-S786, a cephalosporin with broad-spectrum antibacterial activity.
Biological and physicochemical properties of BL-S786 were compared with those of cephalothin, cephaloridine, and cefazolin. With few exceptions, BL-S786 was more active than the reference compounds against major gram-negative pathogenic species and its antibacterial spectrum was broader than that of cephalosporins currently available for clinical use. Although BL-S786 was generally less active than the control cephalosporins against gram-positive pathogens, it inhibited their growth at concentrations that should readily be achieved in humans after standard parenteral dosage. Streptococcus faecalis, a species relatively unsusceptible to cephalosporins in general, was an exception. BL-S786 was an effective bactericidal agent for strains of various gram-negative organisms. After intramuscular administration to mice, BL-S786 achieved high concentrations in blood, and its biological half-life was longer than that of the other three cephalosporins.
D000818:Animals; D001424:Bacterial Infections / Q000188:drug therapy; D001798:Blood Proteins / Q000378:metabolism; D002437:Cefazolin / Q000494:pharmacology; D002509:Cephaloridine / Q000494:pharmacology; D002510:Cephalosporinase / Q000378:metabolism; D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D002512:Cephalothin / Q000494:pharmacology; D004755:Enterobacteriaceae / Q000187:drug effects; D006207:Half-Life; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D011485:Protein Binding; D051381:Rats
D001798:Blood Proteins; D002511:Cephalosporins; D002510:Cephalosporinase; D002437:Cefazolin; D002509:Cephaloridine; D002512:Cephalothin