Microbial transformations of antimicrobial quinolones and related drugs
Igor A Parshikov1, John B Sutherland
1First Moscow State Medical University of I. M. Sechenov, Moscow, Russia.
Abstract:
The quinolones are an important group of synthetic antimicrobial drugs used for treating bacterial diseases of humans and animals. Microorganisms transform antimicrobial quinolones (including fluoroquinolones) and the pharmacologically related naphthyridones, pyranoacridones, and cinnolones to a variety of metabolites. The biotransformation processes involve hydroxylation of methyl groups; hydroxylation of aliphatic and aromatic rings; oxidation of alcohols and amines; reduction of carboxyl groups; removal of methyl, carboxyl, fluoro, and cyano groups; addition of formyl, acetyl, nitrosyl, and cyclopentenone groups; and cleavage of aliphatic and aromatic rings. Most of these reactions greatly reduce or eliminate the antimicrobial activity of the quinolones.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Drug Biotransformation: Overview
Drug Biotransformation: Overview
Gene Regulation in Microbial Communities: Quorum Sensing
Transformation
Mechanism of Antibiotic Resistance in MRSA

