Laboratory evaluation of 3-(5-tetrazolyl) penam, a new semisynthetic beta-lactam antibacterial agent with extended broad-spectrum activity.

Abstract

In the new agent 3-(5-tetrazolyl)penam, hereafter referred to as CP-35,587, the carboxyl function at C3 in the penicillin nucleus has been replaced with the 5-tetrazolyl moiety. Marked changes in spectrum and resistance to gram-negative beta-lactamases, particularly with regard to Klebsiella pneumoniae isolates, were conferred by this modification. The anti-Klebsiella activity clearly distinguishes the antibacterial spectrum of CP-35,587 from any known broad-spectrum penicillin. Compared to orally active cephalosporins, the spectrum advantage of CP-35,587 encompasses Enterobacter, Serratia marcescens, Citrobacter, Providencia, Haemophilus influenzae, and Streptococcus faecalis, both in vitro and in murine infections produced by many of the above-named microorganisms. Thus, CP-35,587 combines and extends the antibacterial activity of broad-spectrum penicillins and orally active cephalosporins.

• Authors: A R English, J A Retsema, J E Lynch
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 10 Issue 1 Pg. 132-8 (Jul 1976) ISSN: 0066-4804 [Print] United States
• PMID: 984745 (Publication Type: Journal Article)

Chemical References

• Blood Proteins
• Penicillins
• Tetrazoles
• beta-Lactamase Inhibitors
• 3-(5-tetrazolyl)penam

Topics

• Animals
• Bacteria (drug effects)
• Bacterial Infections (drug therapy)
• Blood Proteins (metabolism)
• Dogs
• Mice
• Penicillins (metabolism, pharmacology, therapeutic use)
• Protein Binding
• Tetrazoles (metabolism, pharmacology, therapeutic use)
• beta-Lactamase Inhibitors