Recent development in fluorinated antibiotics

Abstract

This chapter presents the most recent results in the development of fluorinated antibioticsby taking into consideration modern challenges of multidrug-resistant pathogens. After a brief introduction on the direct and indirect effects of fluorine and fluorinated moieties in regulating biological activity, the chapter is developed in three main subsections discussing the two major classes of fluorinated antibiotics, fluoroquinolones and oxazolidinones, plus an overview of recent research on the antibiotic activity of fluorinated analogs of tetracyclines, peptidomimetics, triazoles, and nucleosides. Discussed aspects include: (1) Synthesis and challenges posed by the introduction of fluorinated moieties in specific positions of the main scaffold; (2) mechanism of action and structure–activity relationships in which the introduction or modification of fluorinated substituent is crucial to control efficacy; and (3) resistance mechanisms and solutions to treat resistant pathogens.