254882-54-7Relevant academic research and scientific papers
Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa
Renau, Thomas E.,Leger, Roger,Filonova, Lubov,Flamme, Eric M.,Wang, Michael,Yen, Rose,Madsen, Deidre,Griffith, David,Chamberland, Suzanne,Dudley, Michael N.,Lee, Ving J.,Lomovskaya, Olga,Watkins, William J.,Ohta, Toshiharu,Nakayama, Kiyoshi,Ishida, Yohei
, p. 2755 - 2758 (2007/10/03)
Conformational restriction of the ornithine residue of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02,595, 2) furnished bioisosteric proline derivatives that were less toxic in vivo and as active as the lead in potentiat
The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitors
Watkins, William J.,Landaverry, Yakira,Leger, Roger,Litman, Renee,Renau, Thomas E.,Williams, Nicole,Yen, Rose,Zhang, Jason Z.,Chamberland, Suzanne,Madsen, Deidre,Griffith, David,Tembe, Vrushali,Huie, Keith,Dudley, Michael N.
, p. 4241 - 4244 (2007/10/03)
Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series. Upon in
Efflux pump inhibitors
-
, (2008/06/13)
Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.
Addressing the stability of C-capped dipeptide efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa
Renau, Thomas E,Leger, Roger,Flamme, Eric M,She, Miles W,Gannon, Carla L,Mathias, Kristina M,Lomovskaya, Olga,Chamberland, Suzanne,Lee, Ving J,Ohta, Toshiharu,Nakayama, Kiyoshi,Ishida, Yohei
, p. 663 - 667 (2007/10/03)
Synthetic optimization of a biologically labile class of dipeptides that function as efflux pump inhibitors to potentiate the antibacterial agent levofloxacin in Pseudomonas aeruginosa has led to the discovery of a related series of compounds that are completely stable in a variety of biological matrices. Other than the stability profile, the in vitro profile of the new series is essentially identical to that observed with the original one. A prototypical compound from the new series demonstrates potentiation in an in vivo model of infection.
