Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus

Robert J Kerns; Michael J Rybak; Glenn W Kaatz; Flamur Vaka; Raymond Cha; Richard G Grucz; Veena U Diwadkar

doi:10.1016/S0960-894X(03)00376-7

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Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus

Journal article

Peer reviewed

Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus

Robert J Kerns, Michael J Rybak, Glenn W Kaatz, Flamur Vaka, Raymond Cha, Richard G Grucz and Veena U Diwadkar

Bioorganic & medicinal chemistry letters, Vol.13(13), pp.2109-2112

07/07/2003

DOI: 10.1016/S0960-894X(03)00376-7

PMID: 12798315

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Abstract

We previously demonstrated that piperazinyl-linked fluoroquinolone dimers possess potent antibacterial activity against drug-resistant strains of Staphylococcus aureus. In this study, we report the preparation and evaluation of a series of incomplete dimers toward ascertaining structural features of piperazinyl-linked ciprofloxacin dimers that render these agents refractory to fluoroquinolone-resistance mechanisms in Staphylococcus aureus.

Anti-Infective Agents - chemical synthesis

Anti-Infective Agents - chemistry

Anti-Infective Agents - pharmacology

Chromatography, High Pressure Liquid

Chromatography, Thin Layer

Ciprofloxacin - chemical synthesis

Ciprofloxacin - chemistry

Ciprofloxacin - pharmacology

DNA, Bacterial - drug effects

Drug Resistance, Bacterial

Mutation - genetics

Pipemidic Acid - chemical synthesis

Pipemidic Acid - pharmacology

Piperazines - chemical synthesis

Piperazines - chemistry

Piperazines - pharmacology

Staphylococcus aureus - drug effects

Staphylococcus aureus - enzymology

Staphylococcus aureus - genetics

Structure-Activity Relationship

Topoisomerase I Inhibitors

Topoisomerase II Inhibitors

Details

Title: Subtitle: Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus
Creators: Robert J Kerns - Division of Medicinal and Natural Products Chemistry, The University of Iowa, 52242, Iowa City, IA, USA. robert-kerns@uiowa.edu
Michael J Rybak - Wayne State University
Glenn W Kaatz - Wayne State University
Flamur Vaka - Wayne State University
Raymond Cha - Wayne State University
Richard G Grucz - Wayne State University
Veena U Diwadkar - Wayne State University
Resource Type: Journal article
Publication Details: Bioorganic & medicinal chemistry letters, Vol.13(13), pp.2109-2112
DOI: 10.1016/S0960-894X(03)00376-7
PMID: 12798315
ISSN: 0960-894X
eISSN: 1464-3405
Language: English
Date published: 07/07/2003
Academic Unit: Pharmaceutical Sciences and Experimental Therapeutics; Medicinal and Natural Products Chemistry
Record Identifier: 9984366018702771

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