Results 281 to 290 of about 147,157 (321)

Development of efflux pump inhibitors in antituberculosis therapy

International Journal of Antimicrobial Agents, 2016
Resistance and tolerance to antituberculosis (anti-TB) drugs, especially the first-line drugs, has become a serious problem in anti-TB therapy. Efflux of antimicrobial agents via bacterial efflux pumps is one of the main reasons for drug resistance.
Lele, Song, Xueqiong, Wu
openaire   +2 more sources

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

Synthesis of amides from (E)-3-(1-chloro-3,4-dihydronaphthalen-2-yl)acrylic acid and substituted amino acid esters as NorA efflux pump inhibitors of Staphylococcus aureus.

Bioorganic & Medicinal Chemistry, 2019
Inhibitors for NorA efflux pump of Staphylococcus aureus have attracted the attention of many researchers towards the discovery and development of novel efflux pump inhibitors (EPIs).
S. K. Rath, Samsher Singh, Sunil Kumar, N. A. Wani, R. Rai, S. Koul, I. Khan, Payare L. Sangwan   +7 more
semanticscholar   +1 more source

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
openaire   +2 more sources

Tackling drug resistance with efflux pump inhibitors: from bacteria to cancerous cells

Critical reviews in microbiology, 2019
Drug resistance is a serious concern in a clinical setting jeopardizing treatment for both infectious agents and cancers alike. The wide-spread emergence of multi-drug resistant (MDR) phenotypes from bacteria to cancerous cells necessitates the need to ...
Rene Christena Lowrence, Selva Ganesan Subramaniapillai, Venkatasubramanian Ulaganathan, Saisubramanian Nagarajan   +3 more
semanticscholar   +1 more source

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

2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction.

Journal of Medicinal Chemistry, 2018
Antimicrobial resistance (AMR) represents a hot topic in drug discovery. Besides the identification of new antibiotics, the use of nonantibiotic molecules to block resistance mechanisms is a powerful alternative.
Tommaso Felicetti, Rolando Cannalire, D. Pietrella, G. Latacz, Annamaria Lubelska, Giuseppe Manfroni, M. Barreca, Serena Massari, O. Tabarrini, K. Kieć‐Kononowicz, B. Schindler, G. Kaatz, V. Cecchetti, S. Sabatini   +13 more
semanticscholar   +1 more source