A series of cephalosporins has been prepared in which the 3'-position was linked to the nitrogen of the antibacterial quinolone ciprofloxacin through a carbamate function. Like the ester-linked and quaternary-linked dual-action cephalosporins reported earlier, these carbamate-linked compounds exhibited a broad antibacterial spectrum derived from both cephalosporin-like and quinolone-like activities, suggesting a dual mode of action. Studies to elucidate details of the mechanism of action have been inconclusive. Ciprofloxacin liberated as a consequence of bacterial enzyme-mediated reactions may contribute to the second mode of action, although some evidence indicates that the intact carbamate-linked bifunctional molecules may possess intrinsically both beta-lactam and quinolone activities.
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http://dx.doi.org/10.1021/jm00113a026 | DOI Listing |
Colloids Surf B Biointerfaces
June 2020
Bomin Electronics Ltd, Meizhou 514021, China.
Two drugs (cefpirome, cefixime) as dual-action inhibitors could self-organize on copper surface forming bio-functional protective film, which effectively prevents copper corrosion in the picking process with an excellent performance on the resistance of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus).
View Article and Find Full Text PDFAntimicrob Agents Chemother
January 2019
Wockhardt Limited, Mumbai, India.
WCK 5222 is a novel β-lactam-β-lactam-enhancer combination of cefepime (FEP) and zidebactam (ZID). ZID is a novel β-lactam enhancer with a dual action of binding to Gram-negative penicillin-binding protein 2 (PBP2) and β-lactamase inhibition. WCK 5222 is being developed as a new therapeutic option for the treatment of complicated multidrug-resistant Gram-negative pathogen infections.
View Article and Find Full Text PDFAntimicrob Agents Chemother
May 2017
JMI Laboratories, North Liberty, Iowa, USA.
WCK 5222 consists of cefepime combined with zidebactam, a bicyclo-acyl hydrazide β-lactam enhancer antibiotic with a dual action involving binding to Gram-negative bacterial PBP2 and β-lactamase inhibition. We evaluated the activity of cefepime-zidebactam against 7,876 contemporary (2015) clinical isolates of ( = 5,946), ( = 1,291), and spp. ( = 639) from the United States ( = 2,919), Europe ( = 3,004), the Asia-Pacific ( = 1,370), and Latin America ( = 583).
View Article and Find Full Text PDFAntimicrob Agents Chemother
October 2016
Centre d'Ingénierie des Protéines, Université de Liège, Liège, Belgium
β-Lactamases are the most important mechanisms of resistance to the β-lactam antibacterials. There are two mechanistic classes of β-lactamases: the serine β-lactamases (SBLs) and the zinc-dependent metallo-β-lactamases (MBLs). Avibactam, the first clinically useful non-β-lactam β-lactamase inhibitor, is a broad-spectrum SBL inhibitor, which is used in combination with a cephalosporin antibiotic (ceftazidime).
View Article and Find Full Text PDFDrug Metab Pharmacokinet
November 2008
Department of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI 48109-5633, USA.
Pept2 knockout mice are an important tool to evaluate the evolving role and relevance of this proton-coupled oligopeptide transporter beyond drug disposition, where the transporter also modulates the pharmacodynamic and toxicodynamic effects of drug substrates. Our in vivo studies with glycylsarcosine in Pept2 knockout mice have established "proof of concept" that PEPT2 can have a significant effect on dipeptide disposition. Subsequent studies with the aminocephalosporin antibiotic cefadroxil have shown relevance to pharmacology and infectious disease.
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