title: Antibacterial activity of enrofloxacin and ciprofloxacin derivatives of β-octaarginine.
abstract: β(3) -Octaarginine chains were attached to the functional groups NH and CO2 H of the antibacterial fluoroquinolones ciprofloxacin (→1) and enrofloxacin (→2), respectively, in order to find out whether the activity increases by attachment of the polycationic, cell-penetrating peptide (CPP) moiety. For comparison, simple amides, 3-5, of the two antimicrobial compounds and β(3) -octaarginine amide (βR8 ) were included in the antibacterial susceptibility tests to clarify the impact of chemical modification on the microbiological activity of either scaffold (Table).
authors: Laboratorium für Organische Chemie, Departement Chemie und Angewandte Biowissenschaften, ETH-Zürich, Hönggerberg HCI, Vladimir-Prelog-Weg 3, CH-8093 Zürich, (phone: +41-44-632-2990; fax: +41-44-632-1144); Present address: Clariant Produkte GmbH, Competence Center Surfactants, DE-84508 Burgkirchen.
authors: Nirupam
authors: N
authors: Purkayastha
authors: Stefania
authors: S
authors: Capone
authors: Albert K
authors: AK
authors: Beck
authors: Dieter
authors: D
authors: Seebach
authors: Jennifer
authors: J
authors: Leeds
authors: Katherine
authors: K
authors: Thompson
authors: Heinz E
authors: HE
authors: Moser
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D001665:Binding Sites; D057846:Cell-Penetrating Peptides / Q000737:chemistry*; D002939:Ciprofloxacin / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D027081:DNA Gyrase / Q000737:chemistry / Q000378:metabolism; D000077422:Enrofloxacin; D024841:Fluoroquinolones / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D009842:Oligopeptides / Q000737:chemistry*; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D057846:Cell-Penetrating Peptides; D024841:Fluoroquinolones; D009842:Oligopeptides; C448619:octaarginine; D000077422:Enrofloxacin; D002939:Ciprofloxacin; D027081:DNA Gyrase
keywords: Antibacterial activity; Ciprofloxacin derivatives; Enrofloxacin derivatives; β3-Octaarginine derivatives