Premium
Cover Picture: Searching for Novel Inhibitors of the S. aureus NorA Efflux Pump: Synthesis and Biological Evaluation of the 3‐Phenyl‐1,4‐benzothiazine Analogues (ChemMedChem 16/2017)
Author(s) -
Felicetti Tommaso,
Cannalire Rolando,
Burali Maria Sole,
Massari Serena,
Manfroni Giuseppe,
Barreca Maria Letizia,
Tabarrini Oriana,
Schindler Bryan D.,
Sabatini Stefano,
Kaatz Glenn W.,
Cecchetti Violetta
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700470
Subject(s) - efflux , antibiotics , trojan horse , bacteria , chemistry , antibiotic resistance , trojan , antimicrobial , microbiology and biotechnology , biology , biochemistry , computer security , computer science , genetics
The front cover picture shows the everlasting fight between bacteria and humans. Bacteria, which have lost their susceptibility to antimicrobials, are able to survive in the host like Trojan warriors, resisting almost all our weapons. In this bloody war, efflux pump overexpression plays a key role in conferring resistance to a variety of antibacterials. Compounds able to inhibit such pumps (e.g., efflux pump inhibitors or EPIs) act as Trojan horses thus giving new life to old antibacterial agents. Indeed, EPIs should both allow the antibacterials to reach their intracellular target, hence killing the pathogen, and simultaneously be devoid of any antibacterial activity so as not to induce further resistance phenomena. More information can be found in the Full Paper by Stefano Sabatini et al. on page 1293 in Issue 16, 2017 (DOI: 10.1002/cmdc.201700286).