The Quinolones: Past, Present, and Future

Abstract

The quinolone class of antimicrobial agents has generated considerable interest since its discovery >40 years ago. Substantial progress has been made in our understanding of the molecular mechanisms of the action of quinolones against pathogenic bacteria, the induction of resistance to quinolones in these organisms, and the potential of each quinolone compound to induce toxicity in treated patients. Here, these key discoveries are reviewed; the present indications approved by regulatory agencies are described in detail, with comments on adverse events caused by quinolones in treated patients; and speculation about the future of the quinolones is proffered, even though their future is difficult to predict, because many factors may affect their clinical usefulness. However, the emergence of bacterial resistance to the quinolones is a major factor that will determine the future clinical effectiveness of these agents, so that intense investigation of mechanisms to either prevent or curtail resistance to quinolones is of prime importance to their future.

Environmental phosphate differentially affects virulence phenotypes of uropathogenicEscherichia coliisolates causative of prostatitis

“…48 Fluoroquinolones have been the antimicrobial treatment of choice in febrile and acute UTIs. [49][50][51][52] Thus, susceptibility to nalidixic acid and ciprofloxacin was tested. From the 55 isolates tested, 83% and 36% were sensitive to ciprofloxacin and nalidixic acid, respectively.…”

Fluoroquinolone interactions with Mycobacterium tuberculosis gyrase: Enhancing drug activity against wild-type and resistant gyrase

“…Fluoroquinolones are broad-spectrum antibacterial agents that act by increasing levels of DNA strand breaks generated by type II topoisomerases (7)(8)(9)(10)(11)(12). Most bacterial species encode two type II enzymes, gyrase and topoisomerase IV (8,10,(12)(13)(14).…”

Design, Synthesis and Antibacterial Evaluation of Some New 2-Phenyl-quinoline-4-carboxylic Acid Derivatives

“…The quinoline ring occurs in various natural products and represents a key motif in medicinal chemistry [9][10][11][12], and its derivatives, quinoline-4-carboxylic acids, are a group of compounds associated with different biological activities, such asantiviral [13], anti-inflammatory [14], antimicrobial [15], anti-atherothrombosis [16], antiemetic [17], anxiolytic [18], antimalarial and antileishmanial [19]. Although quinoline-4-carboxylic acid derivatives exhibit various bioactivities, the research of new quinoline-4-carboxylic acid-based antibacterial drugs has developed slowly.…”