Home About us MoEF Contact us Sitemap Tamil Website  
About Envis
Whats New
Microorganisms
Research on Microbes
Database
Bibliography
Publications
Library
E-Resources
Microbiology Experts
Events
Online Submission
Access Statistics

Site Visitors

blog tracking


 
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.

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 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).

Copyright © 2005 ENVIS Centre ! All rights reserved
This site is optimized for 1024 x 768 screen resolution