A New Cephalosporin with a Dual Mode of Action
Open Access
- 1 August 1976
- journal article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 10 (2), 245-248
- https://doi.org/10.1128/aac.10.2.245
Abstract
A cephalosporin, (6R,7R)-7-[(2R)-2-hydroxy-2-phenylacetamido]-3-(pyrid-2-yl- N -oxide) thiomethylceph-3-em-4-carboxylic acid (MCO), that could lead to a novel approach to the problem of β-lactamase destruction is described. The compound is slightly more resistant to some β-lactamases than is cephalothin, but it is still hydrolyzed by many to a varying degree. Hydrolysis of the β-lactam bond of a cephalosporin releases the 3-substituent, which in MCO is itself an antibacterial agent, 2-mercaptopyridine- N -oxide. Thus, MCO has a dual mode of action, and bacteria that do not produce an effective amount of a β-lactamase are inhibited by the intact cephalosporin, whereas those that do hydrolyze it are inhibited by the released antibacterial compound.Keywords
This publication has 7 references indexed in Scilit:
- Cefuroxime - A new cephalosporin antibiotic.The Journal of Antibiotics, 1976
- Laboratory tests of antifungal drugs.Journal of Clinical Pathology, 1975
- The β-Lactamases of Gram-Negative Bacteria and their Possible Physiological RolePublished by Elsevier BV ,1973
- Novel Method for Detection of β-Lactamases by Using a Chromogenic Cephalosporin SubstrateAntimicrobial Agents and Chemotherapy, 1972
- Biological Properties of Three 3-Heterocyclic-Thiomethyl Cephalosporin AntibioticsAntimicrobial Agents and Chemotherapy, 1972
- Products of aminolysis and enzymic hydrolysis of the cephalosporinsBiochemical Journal, 1970
- Toxicology of hydroxypyridinethioneToxicology and Applied Pharmacology, 1960