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Bioorganic & Medicinal Chemistry
Vol. 24 (22), 2016, Pages: 6012–6020

Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers

Ekaterina A. Burakova, Irina V. Saranina, Nina V. Tikunova, Zhanna K. Nazarkina, Pavel P. Laktionov, Luboví A. Karpinskaya, Vadim B. Anikin, Vladimir V. Zarubaev, Vladimir N. Silnikov

Institute of Chemical Biology and Fundamental Medicine, Lavrent’ev Ave. 8, Novosibirsk 630090, Russia.


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 2 h. Furthermore, compounds 1ac with aromatic linkers and compound 1e showed the highest antiviral activity.

Graphical abstract

Keywords: Antimicrobial activity; Antiviral activity; Cytotoxicity; 1,4-Diazabicyclo[2.2.2]octane (DABCO); Quaternary ammonium compounds (QACs).

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