Pyrazolo[4,3-c][1,2]benzothiazines 5,5-Dioxide: A Promising New Class of Staphylococcus aureus NorA Efflux Pump Inhibitors

2012 ◽  
Vol 55 (7) ◽  
pp. 3568-3572 ◽  
Author(s):  
Stefano Sabatini ◽  
Francesca Gosetto ◽  
Serena Serritella ◽  
Giuseppe Manfroni ◽  
Oriana Tabarrini ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Efflux Pump ◽  
New Class ◽  
Efflux Pump Inhibitors

Virtual Screening for Novel Staphylococcus Aureus NorA Efflux Pump Inhibitors From Natural Products

2015 ◽  
Vol 11 (2) ◽  
pp. 135-155 ◽  
Author(s):  
Khac-Minh Thai ◽  
Trieu-Du Ngo ◽  
Thien-Vy Phan ◽  
Thanh-Dao Tran ◽  
Ngoc-Vinh Nguyen ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Natural Products ◽  
Virtual Screening ◽  
Efflux Pump ◽  
Efflux Pump Inhibitors

Novel DiOC3 96-well real-time efflux assay for discovery of NorA efflux pump inhibitors in Staphylococcus aureus

2021 ◽  
Vol 181 ◽  
pp. 106128
Author(s):  
Najoua Elhidar ◽  
Ahmed Nafis ◽  
André Goehler ◽  
Abdelaziz Abbad ◽  
Lahcen Hassani ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Real Time ◽  
Efflux Pump ◽  
Efflux Pump Inhibitors

An Update on Staphylococcus aureus NorA Efflux Pump Inhibitors

2020 ◽  
Vol 20 (24) ◽  
pp. 2168-2185
Author(s):  
Kadja Luana Chagas Monteiro ◽  
Thiago Mendonça de Aquino ◽  
Francisco Jaime B. Mendonça Junior
Keyword(s):  
Staphylococcus Aureus ◽  
Bacterial Resistance ◽  
Efflux Pump ◽  
Control Strategies ◽  
Structural Diversity ◽  
Multidrug Resistant ◽  
Efflux Pump Inhibitors ◽  
Vancomycin Resistant ◽  
Sulfur Containing ◽  
Substantial Degree

Background: Methicillin-resistant and vancomycin-resistant Staphylococcus aureus are pathogens causing severe infectious diseases that pose real public health threats problems worldwide. In S. aureus, the most efficient multidrug-resistant system is the NorA efflux pump. For this reason, it is critical to identify efflux pump inhibitors. Objective: In this paper, we present an update of the new natural and synthetic compounds that act as modulators of antibiotic resistance through the inhibition of the S. aureus NorA efflux pump. Results: Several classes of compounds capable of restoring the antibiotic activity have been identified against resistant-S. aureus strains, acting as NorA efflux pump inhibitors. The most promising classes of compounds were quinolines, indoles, pyridines, phenols, and sulfur-containing heterocycles. However, the substantial degree structural diversity of these compounds makes it difficult to establish good structure- activity correlations that allow the design of compounds with more promising activities and properties. Conclusion: Despite substantial efforts put forth in the search for new antibiotic adjuvants that act as efflux pump inhibitors, and despite several promising results, there are currently no efflux pump inhibitors authorized for human or veterinary use, or in clinical trials. Unfortunately, it appears that infection control strategies have remained the same since the discovery of penicillin, and that most efforts remain focused on discovering new classes of antibiotics, rather than trying to prolong the life of available antibiotics, and simultaneously fighting mechanisms of bacterial resistance.

scholarly journals Homology modeling, molecular dynamics, and virtual screening of NorA efflux pump inhibitors of Staphylococcus aureus

2016 ◽  
Vol Volume 10 ◽  
pp. 3237-3252 ◽  
Author(s):  
Baki Vijaya Bhaskar ◽  
Tirumalasetty Muni Chandra Babu ◽  
Netala Vasudeava Reddy ◽  
Wudayagiri Rajendra
Keyword(s):  
Molecular Dynamics ◽  
Staphylococcus Aureus ◽  
Virtual Screening ◽  
Homology Modeling ◽  
Efflux Pump ◽  
Efflux Pump Inhibitors

scholarly journals Corrigendum: Synthesis and Evaluation of 2‐Aminothiophene Derivatives as Staphylococcus aureus Efflux Pump Inhibitors

ChemMedChem ◽  
2021 ◽  
Author(s):  
Rayssa M. D. Cruz ◽  
Renaud Zelli ◽  
Sarah Benshain ◽  
Ryldene M. D. Cruz ◽  
José P. Siqueira‐Júnior ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Efflux Pump ◽  
Efflux Pump Inhibitors

Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position

2018 ◽  
Vol 155 ◽  
pp. 428-433 ◽  
Author(s):  
Tommaso Felicetti ◽  
Rolando Cannalire ◽  
Maria Giulia Nizi ◽  
Oriana Tabarrini ◽  
Serena Massari ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Efflux Pump ◽  
Efflux Pump Inhibitors
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