Author/Authors :
Thomas E. Renau، نويسنده , , Roger Léger، نويسنده , , Eric M. Flamme، نويسنده , , Miles W. She، نويسنده , , Carla L. Gannon، نويسنده , , Kristina M. Mathias، نويسنده , , Olga Lomovskaya، نويسنده , , Suzanne Chamberland، نويسنده , , Ving J. Lee، نويسنده , , Toshiharu Ohta، نويسنده , , Kiyoshi Nakayama، نويسنده , , Yohei Ishida، نويسنده ,
Abstract :
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.
