Results 261 to 270 of about 54,733 (297)

N-Caffeoylphenalkylamide derivatives as bacterial efflux pump inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
As part of an ongoing project to identify plant natural products as efflux pump inhibitors (EPIs), bioassay-guided fractionation of the methanolic extract of Mirabilis jalapa Linn. (Nyctaginaceae) led to the isolation of an active polyphenolic amide: N-trans-feruloyl 4'-O-methyldopamine.
Michalet, Serge, Cartier, Gilbert, David, Bruno, Mariotte, Anne-Marie, Dijoux-Franca, Marie-Geneviève, Kaatz, Glenn, Stavri, Michael, Gibbons, Simon   +7 more
openaire   +4 more sources

An Update on Staphylococcus aureus NorA Efflux Pump Inhibitors

Current Topics in Medicinal Chemistry, 2020
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:
Kadja Luana Chagas, Monteiro, Thiago Mendonça, de Aquino, Francisco Jaime B, Mendonça Junior   +2 more
openaire   +2 more sources

Efflux pump inhibitors reduce the invasiveness of Pseudomonas aeruginosa

International Journal of Antimicrobial Agents, 2009
Efflux systems are thought to contribute to antimicrobial resistance in Pseudomonas aeruginosa. The mexAB-oprM deletion strain of P. aeruginosa PAO1 is compromised in its capacity to invade Madin-Darby canine kidney (MDCK) cells, suggesting that P. aeruginosa exports invasion determinants using a MexAB-OprM system.
Yoichi, Hirakata, Akira, Kondo, Kazuki, Hoshino, Hisakazu, Yano, Kazuaki, Arai, Ayako, Hirotani, Hiroyuki, Kunishima, Natsuo, Yamamoto, Masumitsu, Hatta, Miho, Kitagawa, Shigeru, Kohno, Mitsuo, Kaku   +11 more
openaire   +2 more sources

Inhibitors of Efflux Pumps

Multidrug-resistant bacteria are a major public health threat. MDR efflux pump overexpression and enzymatic changes are major antibiotic resistance mechanisms. Many drug and biofilm resistance strategies involve efflux pumps. Natural substrate and inhibitor identification is a new study. Efflux pump inhibition allows medication buildup inside bacterial
Neeraj Kumar, Sudeshna Bhattacharjee, Rama Tyagi   +2 more
openaire   +1 more source

Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor

Expert Review of Anticancer Therapy, 2007
P-glycoprotein actively transports structurally unrelated compounds out of cells, conferring the multidrug resistance phenotype in cancer. Tariquidar is a potent, specific, noncompetitive inhibitor of P-glycoprotein. Tariquidar inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from the inhibition of ...
Elizabeth, Fox, Susan E, Bates
openaire   +2 more sources

Multidrug Efflux Pumps Attenuate the Effect of MGMT Inhibitors

Molecular Pharmaceutics, 2015
Various mechanisms of drug resistance attenuate the effectiveness of cancer therapeutics, including drug transport and DNA repair. The DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) is a key factor determining the resistance against alkylating anticancer drugs inducing the genotoxic DNA lesions O(6)-methylguanine and O(6 ...
Karl-Heinz, Tomaszowski, Ralf, Schirrmacher, Bernd, Kaina   +2 more
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Substituted dihydronaphthalenes as efflux pump inhibitors of Staphylococcus aureus

European Journal of Medicinal Chemistry, 2010
A new series of 3-(substituted-3,4-dihydronaphthyl)-2-propenoic acid amides has been prepared through convergent synthetic strategies and tested in combination with ciprofloxacin against NorA overexpressing Staphylococcus aureus 1199B as test strain for potentiating of the drug activity.
Thota, Niranjan, Reddy, Mallepally V, Kumar, Ashwani, Khan, Inshad A, Sangwan, Payare L, Kalia, Nitin P, Koul, Jawahir L, Koul, Surrinder   +7 more
openaire   +3 more sources

Efflux pump inhibitors of clinically relevant multidrug resistant bacteria

Medicinal Research Reviews, 2019
AbstractBacterial infections are an increasingly serious issue worldwide. The inability of existing therapies to treat multidrug‐resistant pathogens has been recognized as an important challenge of the 21st century. Efflux pumps are important in both intrinsic and acquired bacterial resistance and identification of small molecule efflux pump inhibitors
Andraž Lamut, Lucija Peterlin Mašič, Danijel Kikelj, Tihomir Tomašič   +3 more
openaire   +2 more sources

Determination of the Efflux Pump-Mediated Resistance Prevalence in Pseudomonas aeruginosa, Using an Efflux Pump Inhibitor

Current Microbiology, 2009
In gram negative bacteria, fluoroquinolone resistance is acquired by target mutations in topoisomerase genes or by reducing the permeation of drugs due to the increase in expression of endogenous multidrug efflux pumps that expel structurally unrelated antimicrobial agents.
Abolghasem, Tohidpour, Shahin, Najar Peerayeh, Jalil F, Mehrabadi, Hadi, Rezaei Yazdi   +3 more
openaire   +2 more sources

Tackling multi-drug resistant fungi by efflux pump inhibitors

Biochemical Pharmacology
The emergence of multidrug-resistant fungi is of grave concern, and its infections are responsible for significant deaths among immunocompromised patients. The treatment of fungal infections primarily relies on a clinical class of antibiotics, including azoles, polyenes, echinocandins, polyketides, and a nucleotide analogue.
Kritika Engle, Gautam Kumar
openaire   +2 more sources