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EnglishThis 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.
| Data di pubblicazione: | 2019 |
| Titolo: | Recent development in fluorinated antibiotics |
| Autori: | PACE, Andrea (Corresponding) |
| Citazione: | Palumbo Piccionello, A., Pibiri, I., Buscemi, S., & Pace, A. (2019). Recent development in fluorinated antibiotics. In Fluorine in Life Sciences: Pharmaceuticals, Medicinal Diagnostics, and Agrochemicals Progress in Fluorine Science Series (pp. 213-239). |
| 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. |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1016/B978-0-12-812733-9.00005-2 |
| Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica |
| Appare nelle tipologie: | 2.01 Capitolo o Saggio |
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