Purkayastha Nirupam, Capone Stefania, Beck Albert K, Seebach Dieter, Leeds Jennifer, Thompson Katherine, Moser Heinz E
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.
Chem Biodivers. 2015 Feb;12(2):179-93. doi: 10.1002/cbdv.201400456.
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).
将β(3)-八聚精氨酸链分别连接到抗菌氟喹诺酮类药物环丙沙星（→1）和恩诺沙星（→2）的NH和CO2H官能团上，以探究通过连接聚阳离子细胞穿透肽（CPP）部分是否会提高活性。作为比较，在抗菌药敏试验中纳入了这两种抗菌化合物的简单酰胺（3-5）和β(3)-八聚精氨酸酰胺（βR8），以阐明化学修饰对任何一种支架的微生物活性的影响（表）。
