Quinoline Derivatives as Promising Inhibitors of Antibiotic Efflux Pump in Multidrug Resistant Enterobacter Aerogenes Isolates

Abstract

Efflux pumps protect the bacterial cell by expelling toxic compounds before they reach intracellular targets. Because this mechanism actively contributes to the resistance of a given bacterium to more than one class of antibiotics, molecules that are able to block the relevant efflux pump are of potential significance to combat drug resistance caused by efflux pumps. Different quinoline derivatives including alkoxy, alkylamino, thioalkoxy and chloroquinolines have been previously reported to make Enterobacter aerogenes resistant isolates that over express the mechanism of efflux, noticeably more susceptible to structurally unrelated antibiotics. In addition, various quinoline derivatives significantly increase the intracellular concentration of chloramphenicol as reported with other inhibitors, thereby suggesting the inhibition of the drug transport by AcrAB-TolC pump, which is fully active in the clinicaly resistant isolates investigated. Here, we discuss the respective properties of this molecular family, taking into account the recent insights into the structural data of AcrB pump.

Geraniol Restores Antibiotic Activities against Multidrug-Resistant Isolates from Gram-Negative Species

“…are rapidly becoming the most problematic bacteria to treat due to the expression of MDR phenotypes and nosocomial status (1,3,4). There is a dire need to search for EPIs that are effective in rendering MDR gram-negative bacteria susceptible to antibiotics to which they are initially resistant (6,7,10,12). The aim of this study was to discover EPIs in essential oils obtained from Corsican plants that are effective against efflux systems of gram-negative bacteria.…”

Detection of potential AcrAB-TolC multidrug efflux pump inhibitor in calyces extract of Hibiscus sabdariffa

“…Few compounds were identified as EPIs for AcrAB-TolC, for example: Arylpiperazines were suggested as MDR reversal agent for RND efflux pumps [10], quinolone derivatives were promising EPIs for AcrAB-TolC in Enterobacter aerogenes [11], artesunate enhances the activity of β-lactam antibiotics through inhibition of AcrAB-TolC of E. coli [12], pimozide inhibits the AcrAB-TolC of E. coli [13], and benzothiazoles were identified as potential AcrAB-TolC efflux pump inhibitors (EPIs) in E. coli [14].…”

New Efficient Synthesis of 3-Carboxylquinolines

“…Quinoline derivatives proved to be possessing antimalarial, 1 anti-inflammatory, 2 anticancer, 3 antibiotic, 4 antihypertensive, 5 tyrokinase PDGF-RTK inhibiting agents, 6 anti HIV, 7 DNA binding capability, 8 antitumor activities, 9 and DNA-intercalating carrier 10 activities. In addition to the medicinal significance, multi-substituted quinolines are valuable synthons exploited for the preparation of nanoand mesostructures with enhanced electronic and photonic properties.…”