Antibacterial Activity of Enrofloxacin and Ciprofloxacin Derivatives of β‐Octaarginine |
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| Authors: | Albert K Beck Dieter Seebach Jennifer Leeds Katherine Thompson Heinz E Moser |
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| Institution: | 1. Laboratorium für Organische Chemie, Departement Chemie und Angewandte Biowissenschaften, ETH‐Zürich, H?nggerberg HCI, Vladimir‐Prelog‐Weg 3, CH‐8093 Zürich, (phone: +41‐44‐632‐2990;2. fax: +41‐44‐632‐1144);3. Novartis Institute of Biomedical Research (NIBR), 4560 Horton Street, Emeryville, CA 94608, USA, (phone: +1‐510‐879‐9598) |
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| Abstract: | β3‐Octaarginine chains were attached to the functional groups NH and CO2H 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 β3‐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). |
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| Keywords: | β 3‐Octaarginine derivatives Antibacterial activity Ciprofloxacin derivatives Enrofloxacin derivatives |
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