title: beta-lactam antibiotics derived from nitrogen heterocyclic acetic acids. 2. Cephalosporin derivatives.
abstract: Three cephalosporin derivatives were prepared from 1,4-dihydro-4-oxypyridine-1-acetic acid. These were the 7-aminocephalosporanic acid (7-ACA) derivative and the compounds with 5-methyl-1,3,4-thiadiazol-2-thiol and 1-methyl-1,2,3,4-tetrazole-5-thiol at C-3 of the cephalosporin nucleus. The antibacterial activity of the 7-ACA derivative was comparable to cephalothin, and that of the other two derivatives was comparable to cefazolin. The 7-ACA derivative, compared to cephalothin, was significantly less metabolized, was less protein bound, and had a longer half life.
mesh_terms: D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001681:Biological Assay; D001798:Blood Proteins / Q000378:metabolism; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D008297:Male; D051379:Mice; D011485:Protein Binding
chemical_list: D001798:Blood Proteins; D002511:Cephalosporins