Mecillinam (FL 1060), a 6β-Amidinopenicillanic Acid Derivative: In Vitro Evaluation

Author:

Tybring L.1

Affiliation:

1. Bacteriological Research Department, Leo Pharmaceutical Products, DK-2750 Ballerup, Denmark

Abstract

Mecillinam (formerly called FL 1060), a novel 6β-amidinopenicillanic acid derivative, showed markedly higher activity than ampicillin against clinical isolates of Enterobacteriaceae . The mode of action of mecillinam is different from that of ampicillin and consequently no intrinsic cross-resistance between the two antibiotics was observed. Mecillinam is inactivated by β-lactamases but is generally more stable than ampicillin; thus an apparent cross-resistance exists for strong β-lactamase producers. The protein binding was low and the activity was relatively independent of pH between 5.5 and 8.0. Slow-growing, insensitive variants of Escherichia coli could be selected but these were not stable. The frequency of insensitive variants was affected by the sodium chloride concentration in the medium.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference6 articles.

1. FL 1060: a new beta-lactam antibiotic with novel properties;Greenwood D.;J. Clin. Pathol.,1973

2. 6,-amidinopenicillanic acids-a new group of antibiotics;Lund F.;Nature (London) New Biol.,1972

3. Mechanism of action and development of resistance to a new amidino penicillin;Matsuhashi S.;J. Bacteriol.,1974

4. Light and electron microscopy of the early response of Escherichia coli to a 6,- amidinopenicillanic acid (FL 1060);Melchior N. H.;Acta Pathol. Microbiol. Scand. Sect. B,1973

5. FL 1060, a new penicillin with a unique mode of action;Park J. T.;Biochem. Biophys. Res. Commun.,1973

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