The Quinolones [antikvár]

Preface Most of the new antimicrobial agents that either have been or will be introduced soon for clinical use belong to the quinolone class of antibacterial agents, that is, the newer 4-quinolones, and in particular, the 6-fluorinated piperazinyl derivatives of this class of compounds. The first clinically important member of the quinolone class, naladixic acid, was introduced into medical practice in 1962. Its use was restricted to the treatment of urinary tract infections and it had a limited spectrum of antibacterial activity. Oxolinic acid and cinoxacin were introduced in the 1970s and were alsó restricted to the treatment of urinary tract infections. Shortly thereafter, the development of newer quinolones expanded rapidly, spearheaded by the introduction of a fluorine at the 6-position in the basic quinolone nucleus. This modification in the quinolone nucleus enchanced and broadened the antibacterial activity of these agents and led to the discovery of newer 4-quinolones with antibacterial activities approximately one thousand times that of nalidixic acid. A number of these compounds have been synthesized recently, and that number is expanding rapidly because of the clinical importance of the newer 4-quinolones. Specifically, the development of potent 4-quinolones provides the clinician with the opportunity to treat serious infections caused by antibiotic-resistant bacteria with effective oral therapy. Furthermore, these newer 4-quinolones have excellent distribution into tissues and low incidences of adverse reactions. The intense interest in this class of antibacterial agents by chemists, microbiologists, pharmacologists and clinicians prompted my colleagues and I to attempt to provide new and cogent information on the newer quinolones so that it would be readily available in one volume. I am much indebted to my colleagues, each of whom contributed thorough reviews on the history, chemistry and mechanism of action, in vitro properties, pharmacokinetics, clinical overview, toxicity, adverse effects and drug interactions, and future prospects of the newer 4-quinolones. Our hope is that readers will find this work a ready resource for new and helpful information, and in so doing, the efforts of my colleagues most certainly will have been worthwhile. Vincent T. Andriole, M.D. Yale University School of Medicine