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Title: Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers
Authors: Burakova, Ekaterina A
Saranina, Irina V
Tikunova, Nina V
Nazarkina, Zhanna K
Laktionov, Pavel P
Karpinskaya, Lubov' A
Anikin, Vadim B
Silnikov, Vladimir N
Zarubaev, Vladimir V. 
Keywords: 1,4-Diazabicyclo[2.2.2]octane (DABCO);Antimicrobial activity;Antiviral activity;Cytotoxicity;Quaternary ammonium compounds (QACs)
Issue Date: 2016
Publisher: Elsevier
Journal: Bioorganic and Medicinal Chemistry 
Abstract: A series of 1,4-diazabicyclo[2.2.2]octane derivatives differing by linker moiety was evaluated for activity against several strains of both Gram-positive and Gram-negative bacteria including drug-resistant strains, one strain of fungus and influenza virus A/Puerto Rico/8/34 (H1N1). All compounds exhibited high antibacterial activity against all bacteria except Proteus vulgaris. The minimum inhibitory concentrations (MICs) of compound 1c with an o-phenylenebismethyl linker and compound 1e with a propylene aliphatic linker were found to be low and were comparable or better to the reference drug ciprofloxacin for Pseudomonas aeruginosa and Staphylococcus aureus. Additionally, a time-kill assay was performed to examine the bactericidal kinetics. Compounds 1c and 1e displayed rapid killing effects against St. aureus and Ps. aeruginosa after 2h. Furthermore, compounds 1a-c with aromatic linkers and compound 1e showed the highest antiviral activity.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2016.09.064
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