Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives

Authors

  • Svitlana Danylchenko National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002, Ukraine
  • Oleksandr Drushlyak National University of Pharmacy 53 Pushkinska str., Kharkov, Ukraine, 61002, Ukraine
  • Svitlana Kovalenko National University of Pharmacy 53 Pushkinska str., Kharkov, Ukraine, 61002, Ukraine
  • Sergiy Kovalenko V. N. Karazin Kharkiv National University 4 Svobody squ., Kharkiv, Ukraine, 61022, Ukraine
  • Alysha Elliott The Univercity of Queensland Brisbane QLD 4072 Australia, Australia
  • Johannes Zuegg The Univercity of Queensland Brisbane QLD 4072 Australia, Australia

DOI:

https://doi.org/10.15587/2313-8416.2016.67685

Keywords:

[1, 2, 4]triazolo[4, 3-a]quinazolin-5(4H)-one, antimicrobial activity Escherihia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Cryptococcus neoformans

Abstract

Aim. The aim of the given study was to conduct primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives.

Methods. The set of 169 novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives has been tested for activity against 5 bacteria: Escherihia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa and Staphylococcus aureus, and 2 fungi: Candida albicans and Cryptococcus neoformans. Primary antimicrobial screening has been conducted by whole cell growth inhibition assays, using the provided samples at a single concentration. Samples were tested in water – 0.3 % DMSO solutions with final sample concentrations 32 µg/ml (70-80 µMol).

Results. [1,2,4]Triazolo[4,3-a]quinazolin-5(4H)-ones 5{1}, 7{1}, 7{2}, 7{3} showed more than 80 % inhibition of Acinetobacter baumannii growth and compounds 7{4} showed more than 80 % inhibition of growth fungi Cryptococcus neoformans.

Conclusions. For the first time conducted antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones showed that compounds, which had no amide group exhibited no antimicrobial activity, but several [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives containing amide group attached by carbon or sulfur-carbon chain possess antimicrobial activity against Acinetobacter baumannii or fungi Cryptococcus neoformans

Author Biographies

Svitlana Danylchenko, National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002

Scientific Secretary of scientific and research department

Oleksandr Drushlyak, National University of Pharmacy 53 Pushkinska str., Kharkov, Ukraine, 61002

Candidate of chemical sciences, associate professor

Department of Quality Management

Svitlana Kovalenko, National University of Pharmacy 53 Pushkinska str., Kharkov, Ukraine, 61002

Candidate of chemical sciences, associate professor

Department of Quality Management

Sergiy Kovalenko, V. N. Karazin Kharkiv National University 4 Svobody squ., Kharkiv, Ukraine, 61022

Doctor of chemical sciences, professor

Department of Organic Chemistry

Alysha Elliott, The Univercity of Queensland Brisbane QLD 4072 Australia

Institute for Molecular Bioscience

Johannes Zuegg, The Univercity of Queensland Brisbane QLD 4072 Australia

Institute for Molecular Bioscience

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Published

2016-04-29

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Section

Pharmaceutical Sciences