Enhancement of Antibiotic Activity against Multidrug-Resistant Bacteria by the Efflux Pump Inhibitor 3,4-Dibromopyrrole-2,5-dione Isolated from aPseudoalteromonassp.

2015 ◽  
Vol 78 (3) ◽  
pp. 402-412 ◽  
Author(s):  
Kristen E. Whalen ◽  
Kelsey L. Poulson-Ellestad ◽  
Robert W. Deering ◽  
David C. Rowley ◽  
Tracy J. Mincer
Keyword(s):  
Efflux Pump ◽  
Multidrug Resistant ◽  
Antibiotic Activity ◽  
Resistant Bacteria ◽  
Multidrug Resistant Bacteria ◽  
Efflux Pump Inhibitor

scholarly journals 5-Arylideneimidazolones with Amine at Position 3 as Potential Antibiotic Adjuvants against Multidrug Resistant Bacteria

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 438 ◽  
Author(s):  
Aneta Kaczor ◽  
Karolina Witek ◽  
Sabina Podlewska ◽  
Joanna Czekajewska ◽  
Annamaria Lubelska ◽  
...  
Keyword(s):  
Efflux Pump ◽  
Enterobacter Aerogenes ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Aromatic Rings ◽  
Efflux Pump Inhibitor ◽  
Fold Reduction ◽  
Dual Action ◽  
New Compounds

Searching for new chemosensitizers of bacterial multidrug resistance (MDR), chemical modifications of (Z)-5-(4-chlorobenzylidene)-2-(4-methylpiperazin-1-yl)-3H-imidazol-4(5H)-one (6) were performed. New compounds (7–17), with fused aromatic rings at position 5, were designed and synthesized. Crystallographic X-ray analysis proved that the final compounds (7–17) were substituted with tertiary amine-propyl moiety at position 3 and primary amine group at 2 due to intramolecular Dimroth rearrangement. New compounds were evaluated on their antibiotic adjuvant properties in either Gram-positive or Gram-negative bacteria. Efflux pump inhibitor (EPI) properties towards the AcrAB-TolC pump in Enterobacter aerogenes (EA289) were investigated in the real-time efflux (RTE) assay. Docking and molecular dynamics were applied to estimate an interaction of compounds 6–17 with penicillin binding protein (PBP2a). In vitro ADME-Tox properties were evaluated for compound 9. Most of the tested compounds reduced significantly (4-32-fold) oxacillin MIC in highly resistant MRSA HEMSA 5 strain. The anthracene-morpholine derivative (16) was the most potent (32-fold reduction). The tested compounds displayed significant EPI properties during RTE assay (37–97%). The naphthyl-methylpiperazine derivative 9 showed the most potent “dual action” of both oxacillin adjuvant (MRSA) and EPI (E. aerogenes). Molecular modeling results suggested the allosteric mechanism of action of the imidazolones, which improved binding of oxacillin in the PBP2a active site in MRSA.

Efflux pump inhibitors of clinically relevant multidrug resistant bacteria

2019 ◽  
Vol 39 (6) ◽  
pp. 2460-2504 ◽  
Author(s):  
Andraž Lamut ◽  
Lucija Peterlin Mašič ◽  
Danijel Kikelj ◽  
Tihomir Tomašič
Keyword(s):  
Efflux Pump ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Multidrug Resistant Bacteria ◽  
Efflux Pump Inhibitors

scholarly journals Hospital Wastewater—Important Source of Multidrug Resistant Coliform Bacteria with ESBL-Production

2020 ◽  
Vol 17 (21) ◽  
pp. 7827
Author(s):  
Kristína Lépesová ◽  
Petra Olejníková ◽  
Tomáš Mackuľak ◽  
Klára Cverenkárová ◽  
Monika Krahulcová ◽  
...  
Keyword(s):  
Efflux Pump ◽  
Wastewater Treatment Plants ◽  
Resistance Mechanism ◽  
Multidrug Resistant ◽  
Coliform Bacteria ◽  
Resistant Bacteria ◽  
Hospital Wastewater ◽  
Multidrug Resistant Bacteria ◽  
Antibiotic Resistant ◽  
Extended Spectrum

This work compares the prevalence of antibiotic resistant coliform bacteria in hospital wastewater effluents in Slovak (SR) and Czech Republic (ČR). It also describes selected antibiotic resistant isolates in view of resistance mechanism and virulence factor. The highest number of multidrug resistant bacteria was detected in samples from the hospital in Valašské Meziříčí (ČR). More than half of resistant isolates showed multidrug resistance phenotype as well as strong ability to form biofilm. In 42% of isolates efflux pump overproduction was detected together with tetA and tetE genes. The production of extended-spectrum β-lactamases in coliform isolates was encoded mainly by blaTEM, blaCTX-M-2 and blaCTX-M-8/25 genes. About 62% of resistants contained a combination of two or more extended spectrum beta-lactamases (ESBL) genes. Our results strengthen the fact that hospital effluents are a source of multidrug resistant bacteria which can spread their resistance genes to other bacteria in wastewater treatment plants (WWTPs). Accordingly, hospital wastewater should be better treated before it enters urban sewerage.

C-terminal Lysine-Linked Magainin 2 with Increased Activity Against Multidrug-Resistant Bacteria

2016 ◽  
Vol 23 (8) ◽  
pp. 738-747 ◽  
Author(s):  
Esteban N. Lorenzón ◽  
Norival A. Santos-Filho ◽  
Matheus A. S. Ramos ◽  
Tais M. Bauab ◽  
Ilana L. B. C. Camargo ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Multidrug Resistant Bacteria ◽  
Increased Activity
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