Chemistry & Biodiversity 2015-02-01

Antibacterial activity of enrofloxacin and ciprofloxacin derivatives of β-octaarginine.

Nirupam Purkayastha, Stefania Capone, Albert K Beck, Dieter Seebach, Jennifer Leeds, Katherine Thompson, Heinz E Moser

Index: Chem. Biodivers. 12(2) , 179-93, (2015)

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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). Copyright © 2015 Verlag Helvetica Chimica Acta AG, Zürich.