1462855-83-9Relevant academic research and scientific papers
Glycomimetic, Orally Bioavailable LecB Inhibitors Block Biofilm Formation of Pseudomonas aeruginosa
Sommer, Roman,Wagner, Stefanie,Rox, Katharina,Varrot, Annabelle,Hauck, Dirk,Wamhoff, Eike-Christian,Schreiber, Janine,Ryckmans, Thomas,Brunner, Thomas,Rademacher, Christoph,Hartmann, Rolf W.,Br?nstrup, Mark,Imberty, Anne,Titz, Alexander
, p. 2537 - 2545 (2018)
The opportunistic Gram-negative bacterium Pseudomonas aeruginosa is a leading pathogen for infections of immuno-compromised patients and those suffering from cystic fibrosis. Its ability to switch from planktonic life to aggregates, forming the so-called biofilms, is a front-line mechanism of antimicrobial resistance. The bacterial carbohydrate-binding protein LecB is an integral component and necessary for biofilm formation. Here, we report a new class of drug-like low molecular weight inhibitors of the lectin LecB with nanomolar affinities and excellent receptor binding kinetics and thermodynamics. This class of glycomimetic inhibitors efficiently blocked biofilm formation of P. aeruginosa in vitro while the natural monovalent carbohydrate ligands failed. Furthermore, excellent selectivity and pharmacokinetic properties were achieved. Notably, two compounds showed good oral bioavailability, and high compound concentrations in plasma and urine were achieved in vivo.
INHIBITORS OF PSEUDOMONAS AERUGINOSA LECB
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Page/Page column 75, (2016/10/11)
The present invention relates to compounds derived from deoxy fucose. These compounds are useful as lectin inhibitors, especially as inhibitors of LecB. The invention also relates to pharmaceutical compositions comprising these compounds. The invention further relates to therapeutic uses of these compounds, especially to the prophylaxis or treatment of infections involving Pseudomonas aeruginosa.
GLYCOMIMETICS AS PSEUDOMONAS AERUGINOSA LECTIN INHIBITORS
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, (2013/11/05)
The present invention relates to fucose- and mannose-derived glycomimetics and their general use in prophylaxis or treatment of Pseudomonas aeruginosa infections including respiratory tract infections, urinary tract infections, nosocomial infections and chronic wound infections in a patient encompassing a patient suffering already from cystic fibrosis. Said glycomimetics are inhibitors of Pseudomonas aeruginosa lectin LecB.
