Identification and characterization of an anti-pseudomonal dichlorocarbazol derivative displaying anti-biofilm activity.

Basic Information

ID: ALA3352500

Journal: Bioorg Med Chem Lett

Title: Identification and characterization of an anti-pseudomonal dichlorocarbazol derivative displaying anti-biofilm activity.

Authors: Liebens V, Gerits E, Knapen WJ, Swings T, Beullens S, Steenackers HP, Robijns S, Lippell A, O'Neill AJ, Veber M, Fröhlich M, Krona A, Lövenklev M, Corbau R, Marchand A, Chaltin P, De Brucker K, Thevissen K, Cammue BP, Fauvart M, Verstraeten N, Michiels J.

Abstract: Pseudomonas aeruginosa strains resistant towards all currently available antibiotics are increasingly encountered, raising the need for new anti-pseudomonal drugs. We therefore conducted a medium-throughput screen of a small-molecule collection resulting in the identification of the N-alkylated 3,6-dihalogenocarbazol 1-(sec-butylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol (MIC = 18.5 μg mL⁻¹). This compound, compound 1, is bacteriostatic towards a broad spectrum of Gram-positive and Gram-negative pathogens, including P. aeruginosa. Importantly, 1 also eradicates mature biofilms of P. aeruginosa. 1 displays no cytotoxicity against various human cell types, pointing to its potential for further development as a novel antibacterial drug.

CiteXplore: 25453797

DOI: 10.1016/j.bmcl.2014.10.039

Patent ID: ┄