title: Reversal of Tetracycline Resistance in Escherichia coli by Noncytotoxic bis(Tryptophan)s.
abstract: Nine bis(tryptophan) derivatives (BTs) and two control compounds were synthesized and tested for antimicrobial activity against two Escherichia coli strains and a Staphylococcus aureus strain. The effects of linker type, shape, and conformational rigidity were manifested in dramatic differences in altering tetracycline potency when coadministered with that antibiotic. A reversal of resistance was observed for an E. coli strain having a TetA efflux pump. Survival of mammalian cells was assayed with good result.
authors.affiliation: Center for Nanoscience, Departments of ‡Chemistry & Biochemistry and §Biology, University of Missouri - St. Louis , 1 University Blvd., St. Louis, Missouri 63121, United States.
authors.forename: Joseph W
authors.initials: JW
authors.lastname: Meisel
authors.affiliation: Center for Nanoscience, Departments of ‡Chemistry & Biochemistry and §Biology, University of Missouri - St. Louis , 1 University Blvd., St. Louis, Missouri 63121, United States.
authors.forename: Mohit B
authors.initials: MB
authors.lastname: Patel
authors.affiliation: Center for Nanoscience, Departments of ‡Chemistry & Biochemistry and §Biology, University of Missouri - St. Louis , 1 University Blvd., St. Louis, Missouri 63121, United States.
authors.forename: Evan
authors.initials: E
authors.lastname: Garrad
authors.affiliation: Center for Nanoscience, Departments of ‡Chemistry & Biochemistry and §Biology, University of Missouri - St. Louis , 1 University Blvd., St. Louis, Missouri 63121, United States.
authors.forename: Ryan A
authors.initials: RA
authors.lastname: Stanton
authors.affiliation: Center for Nanoscience, Departments of ‡Chemistry & Biochemistry and §Biology, University of Missouri - St. Louis , 1 University Blvd., St. Louis, Missouri 63121, United States.
authors.forename: George W
authors.initials: GW
authors.lastname: Gokel
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D002463:Cell Membrane Permeability; D004926:Escherichia coli / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013753:Tetracycline Resistance / Q000187:drug effects*; D014364:Tryptophan / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000900:Anti-Bacterial Agents; D014364:Tryptophan