Antibacterial activity of cationic amphiphil conjugates with ciprofloxacin

Danila Zadvornykh; Zhenwei Zhang; Chengjie Liu; Inna Serpokrylovа; Alevtina Bardashevа; Nina Tikunova; Vladimir Silnikov; Lyudmila Koroleva

doi:10.53730/ijhs.v6nS7.12110

Authors

Danila Zadvornykh Novosibirsk State University, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)
Zhenwei Zhang PhD in Chemistry, Teaching and Research Department of Linyi Vocational University of Science and Technology (Linyi Institutes of Industrial Technology)
Chengjie Liu Chemical engineer, Shandong Yangdu Jianhua Pharmaceutical Co., Ltd, Intersection of Yuquan Road and Xiangyang Road, Yinan County, Linyi City, Shandong Province, China
Inna Serpokrylovа PhD in Chemistry, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)
Alevtina Bardashevа Lead Engineer, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)
Nina Tikunova Doctor of Chemical Sciences, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)
Vladimir Silnikov
silnikov_v@ro.ru
Doctor of Chemical Sciences, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)
Lyudmila Koroleva PhD in Chemistry, Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of the Russian Academy of Sciences (ICBFM SB RAS)

Keywords:

chemical synthesis, gram-positive bacteria, gram-negative bacteria

Abstract

The aim: Design and synthesis of new compounds with antibacterial activity. Determination of the minimum inhibitory and minimum bactericidal concentration of conjugates of cationic amphiphiles based on quaternary salts of 1,4-diazabicyclo[2.2.2]octane with ciprofloxacin. Materials and methods: The article is dedicated to the synthesis and primary assessment of antibacterial activity in vitro of conjugates of cationic amphiphiles based on quaternary salts of 1,4-diazabicyclo[2.2.2]octane with ciprofloxacin against gram-negative and gram-positive microorganisms. Results: The present work provides hybrid structures which include the widely used antibiotic ciprofloxacin and tetra-cationic DABCO derivatives. The last ones previously showed a wide spectrum of antimicrobial activity as well as primary studies of their antibacterial activity against gram-positive and gram-negative microorganisms in vitro. There was a high in vitro antibacterial activity against gram-negative pathogens, moderate against Staphylococcus aureus and low against Enterococcus faecalis. Conclusions: A range of amphiphilic polycationic compounds based on quaternary salts of 1,4-diazabicyclo[2.2.2]octane (DABCO) was synthesized and their biological activity was studied. The compounds have demonstrated high antibacterial activity. We assume that they can serve as a basis for the development of new antibacterial drugs.

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