Abstract
Erythromycin, the first antibacterial macrolide introduced into the clinical setting over 50 years ago, was used extensively not only for the treatment of respiratory tract infections in both adults and children, but also for bone and soft tissue infections, and specific sexually transmitted diseases. Macrolide antibiotics have undergone a dramatic chemical evolution over the past 50 years, culminating in the improved 14- and 16-membered macrolides, acylides and new ketolides. In all cases, improvements in antibacterial activity involved changes in the interplay between the chemical structure of the macrolide and the components of the bacterial cell that dictate ultimate antibacterial activity and efficacy. Target site modification by methylation of ribosomal RNA, the so-called Macrolide-Streptogramin-Lincosamide, (MLS0 resistance and active efflux are the two most common forms of resistance present in the clinic today; however, other resistance mechanisms are known. The first macrolide that bound to MLS-resistant ribosomes was reported in 1989, demonstrating that appropriate structural changes could regain access to the modified ribosome-binding site. In addition, macrolide analogs with reduced affinity for the active efflux p...Continue Reading
Citations
Jun 17, 2005·Lipids·Valery M Dembitsky
Jul 11, 2006·The Journal of Biological Chemistry·David H ShermanLarissa M Podust
Nov 8, 2008·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·Jørgen S JensenRyoichi Hamasuna
Sep 5, 2009·Microbial Drug Resistance : MDR : Mechanisms, Epidemiology, and Disease·Lorna A SevilleAdam P Roberts
Jun 19, 2008·Antimicrobial Agents and Chemotherapy·Olga DanilchankaMichael Niederweis
Dec 29, 2011·Antimicrobial Agents and Chemotherapy·Magdalena PopowskaBrion Duffy
Feb 4, 2014·PloS One·Mariangela TaboneJuan C Alonso
Mar 24, 2011·Future Medicinal Chemistry·Robert C Goldman
Feb 6, 2014·The Journal of Antibiotics·Ryuichi SugamataKazuo Suzuki
Nov 8, 2005·FEBS Letters·Li ZhangKimitsuna Watanabe
Oct 15, 2013·Tuberculosis·Robert C Goldman
May 26, 2005·The Journal of Antimicrobial Chemotherapy·Keith Poole
Jun 15, 2006·Expert Review of Anti-infective Therapy·Francesco Scaglione, Luca Paraboni
Feb 7, 2007·Physical Review Letters·Johan ElfMåns Ehrenberg
Nov 29, 2016·Microbiology Insights·Shilpi GuptaDaniel E Kadouri
Jul 15, 2016·ChemMedChem·Joanna DomagalskaPiotr Przybylski
Mar 3, 2009·Chemical Reviews·Jyoti P NandyPrabhat Arya
Mar 11, 2008·Biochemistry·E Sethe Burgie, Hazel M Holden
Feb 27, 2014·Chemical Reviews·Stefano Rizzo, Herbert Waldmann