Abstract
Broad antibacterial spectrum, high oral bioavailability and excellent tissue penetration combined with safety and few, yet rare, unwanted effects, have made the quinolones class of antimicrobials one of the most used in inpatients and outpatients. Initially discovered during the search for improved chloroquine-derivative molecules with increased anti-malarial activity, today the quinolones, intended as antimicrobials, comprehend four generations that progressively have been extending antimicrobial spectrum and clinical use. The quinolone class of antimicrobials exerts its antimicrobial actions through inhibiting DNA gyrase and Topoisomerase IV that in turn inhibits synthesis of DNA and RNA. Good distribution through different tissues and organs to treat Gram-positive and Gram-negative bacteria have made quinolones a good choice to treat disease in both humans and animals. The extensive use of quinolones, in both human health and in the veterinary field, has induced a rise of resistance and menace with leaving the quinolones family ineffective to treat infections. This review revises the evolution of quinolones structures, biological activity, and the clinical importance of this evolving family. Next, updated information regarding the mechanism of antimicrobial activity is revised. The veterinary use of quinolones in animal productions is also considered for its environmental role in spreading resistance. Finally, considerations for the use of quinolones in human and veterinary medicine are discussed.
Highlights
Transmissible diseases kill an estimate of over 15 million people every year worldwide, with many deaths caused by bacterial infections
Flumequine showed an 8-times increased activity against S. aureus [69]. This led to designing molecules that combined the piperazinyl substituent in position 7 and a fluorine atom in position 6 leading to the first fluoroquinolone, norfloxacin, that showed an increase in activity against Gram-negative and Gram-positive bacteria and an improvement in pharmacokinetic, with respect to nalidixic acid [67]
For an in-depth review of their characteristics and their role in therapeutics, we suggest the review by Rusu et al, here they describe introduced modifications that might shape the fifth generations of quinolones [44]
Summary
Transmissible diseases kill an estimate of over 15 million people every year worldwide, with many deaths caused by bacterial infections. Since the origin of quinolones is fully synthetic, they represent a truly synthetic antimicrobial, in opposition to antibiotics which can trace their origin to a natural product. Though the last six decades the quinolones have become one of the most successful antimicrobials from many points of view including but not limited to spectrum, administrations, and tissue distribution. A drug widely used to treat a variety of diseases caused by Gram-negative and Gram-positive bacteria, including respiratory tract infections, urinary infections, and several enteric diseases. As it is for other antibiotics, the use of quinolones is not absent of problems. The impact in the environment and up to date mechanisms of resistance are reviewed before discussing consideration for the use of quinolones to maintain this important family of drugs working against microorganisms
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