The quinolones are synthetic antibiotics derived from nalidixic acid. Chemical modification of basic structure (nalidixic acid) has led to the development of a group of various compounds currently used in medicine. This article discusses the generation of quinolones, mode of their action, and relationship between activity and structure of these antibiotics. The most common quinolones, lomefloxacin and sparfloxacin were discussed in details, also the therapeutic potential of newer agents was reviewed. Recently, understanding of how molecular modifications among quinolone core structure can affect antimicrobial and anticancer activities has progressed rapidly. In this paper we discussed few examples of fluoroquinolone structural modifications. It was proved that many organic and inorganic compounds derived from fluoroquinolones overcame bacterial drug-resistance. Furthermore, chemical modification improved fluoroquinolone’s anticancer activities.
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