Abstract
Macrolide antibiotics are an important class that are used to treat respiratory tract, skin and skin-structure, sexually transmitted, and various other infections. They exert their antimicrobial activity by inhibiting ribosomal protein biosynthesis. Resistance to antibiotics arises when antibiotic binding at its target site is disrupted, efflux pumps remove antibiotic from cells, or antibiotic is converted to an inactive metabolite. Following the isolation of erythromycin and many other macrolides from fermentation broths of soil microbes, three generations of semi-synthetic 14-, 15-, and 16-membered derivatives have been prepared and tested. Two second generation derivatives, clarithromycin and azithromycin, are the more utilized macrolides at this time. Ketolides are third generation derivatives of erythromycin that possess activity against many macrolide-resistant bacteria. Use of the first approved ketolide, telithromycin, has been restricted due to side effects, but some other ketolides have entered into development studies and clinical trials.
Keywords
- Generation Derivative
- Macrolide Antibiotic
- Intramolecular Cyclization
- Exit Tunnel
- Peptidyl Transferase Center
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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Kirst, H.A. (2014). Macrolide Antibiotics. In: Marinelli, F., Genilloud, O. (eds) Antimicrobials. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-39968-8_11
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