Antibacterial Activity of Enrofloxacin and Ciprofloxacin Derivatives of β-Octaarginine)

被引：22

作者：

Purkayastha, Nirupam ^{[1
]}

Capone, Stefania ^{[1
]}

Beck, Albert K. ^{[1
]}

Seebach, Dieter ^{[1
]}

Leeds, Jennifer ^{[2
]}

Thompson, Katherine ^{[2
]}

Moser, Heinz E. ^{[2
]}

机构：

[1] ETH, Dept Chem & Angew Biowissensch, Lab Organ Chem, Honggerberg HCI, CH-8093 Zurich, Switzerland

[2] NIBR, Emeryville, CA 94608 USA

来源：

CHEMISTRY & BIODIVERSITY | 2015年 / 12卷 / 02期

关键词：

(3)-Octaarginine derivatives; Antibacterial activity; Ciprofloxacin derivatives; Enrofloxacin derivatives; CELL-PENETRATING PEPTIDES; IN-VIVO; DNA GYRASE; PERMEABLE PEPTIDES; HUMAN LEUKEMIA; DELIVERY; QUINOLONE; INHIBITION; TARGET; MEMBRANE;

D O I：

10.1002/cbdv.201400456

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

beta(3)-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 (3)-octaarginine amide (R-8) were included in the antibacterial susceptibility tests to clarify the impact of chemical modification on the microbiological activity of either scaffold (Table).

引用

页码：179 / 193

页数：15

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