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ID: ALA1134217

Journal: Bioorg Med Chem Lett

Title: Addressing the stability of C-capped dipeptide efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa.

Authors: Renau TE, Léger R, Flamme EM, She MW, Gannon CL, Mathias KM, Lomovskaya O, Chamberland S, Lee VJ, Ohta T, Nakayama K, Ishida Y.

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.

CiteXplore: 11266165

DOI: 10.1016/s0960-894x(01)00033-6