Biological evaluation of tetracationic compounds based on two 1,4-diazabicyclo[2.2.2]octane moieties connected by different linkers |
| |
| Affiliation: | 1. Institute of Chemical Biology and Fundamental Medicine, Lavrent’ev Ave. 8, Novosibirsk 630090, Russia;2. Influenza Research Institute, Prof. Popova Str. 15/17, St. Petersburg 197376, Russia;1. Department of Biology, Faculty of Science, University of Split, Teslina 12, 21 000 Split, Croatia;2. Department of Chemistry, Faculty of Science, University of Split, Teslina 12, 21 000 Split, Croatia;3. Division of Physical Chemistry, Ruđer Bošković Institute, Bijenička cesta 54, 10 000 Zagreb, Croatia;4. Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, 10 000 Zagreb, Croatia;1. Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center of RAS, Arbuzov str. 8, 420088 Kazan, Russian Federation;2. Kazan Federal University, Kremlevskaya st. 18, 420008 Kazan, Russian Federation;3. Kazan National Research Technical University named after A. N. Tupolev – KAI, K. Marx str. 10, 420111 Kazan, Russian Federation |
| |
| 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 2 h. Furthermore, compounds 1a–c with aromatic linkers and compound 1e showed the highest antiviral activity. |
| |
| Keywords: | Antimicrobial activity Antiviral activity Cytotoxicity 1,4-Diazabicyclo[2.2.2]octane (DABCO) Quaternary ammonium compounds (QACs) |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
