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PMID: 984745 Published · ppublish English Journal Article

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

Antimicrobial agents and chemotherapy ·Vol. 10 ·No. 1 ·1976-07-00 ·Pages 132-8

English AR, Retsema JA, Lynch JE

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.

MeSH Terms
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
Chemicals
Blood Proteins Penicillins Tetrazoles beta-Lactamase Inhibitors 3-(5-tetrazolyl)penam
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
English A R
Retsema J A
Lynch J E
References (4)
4 references, click to expand
  1. MICRO-METHOD FOR INTRAVENOUS INJECTION AND BLOOD SAMPLING.
    J Pharm Sci. 1963 Aug;52:794-5 PMID: 14057900
  2. Carbenicillin indanyl sodium, an orally active derivative of carbenicillin.
    Antimicrob Agents Chemother. 1972 Mar;1(3):185-91 PMID: 4558137
  3. Total synthesis of bisnorpenicillin V.
    J Med Chem. 1974 Apr;17(4):389-92 PMID: 4208535
  4. Micro-iodometric assay for penicillinase.
    Biochem J. 1962 May;83:236-40 PMID: 14480578
Article Info
Journal
Antimicrobial agents and chemotherapy
Abbr.
Antimicrob Agents Chemother
ISSN
0066-4804
Published
1976-07-00
Pages
132-8
Language
English
Region
United States
NLM ID
0315061
PMCID
PMC429702
Subset
IM
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