Antibacterial Activity of Enrofloxacin and Ciprofloxacin Derivatives of β‐Octaarginine1. Issue 2 (February 2015)

• Record Type: Journal Article
• Authors: Purkayastha, Nirupam; Capone, Stefania; Beck, Albert K.; Seebach, Dieter; Leeds, Jennifer; Thompson, Katherine; Moser, Heinz E.
• Is Part Of: Chemistry & biodiversity. Volume 12:Issue 2(2015:Feb.)
• Page Start: 179
• Page End: 193
• Publication Date: 2015-02
• Subjects: Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.201400456
• Languages: English
• ISSNs: 1612-1872

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p> <italic>β</italic> ³‐Octaarginine chains were attached to the functional groups NH and CO₂H of the antibacterial fluoroquinolones ciprofloxacin (→<bold>1</bold>) and enrofloxacin (→<bold>2</bold>), respectively, in order to find out whether the activity increases by attachment of the polycationic, cell‐penetrating peptide (CPP) moiety. For comparison, simple amides, <bold>3</bold>–<bold>5</bold>, of the two antimicrobial compounds and <italic>β</italic>³‐octaarginine amide (<bold><italic>β</italic>R₈</bold>) were included in the antibacterial susceptibility tests to clarify the impact of chemical modification on the microbiological activity of either scaffold (<italic>Table</italic>).</p> </abstract>