Primary antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives
DOI :
https://doi.org/10.15587/2313-8416.2016.67685Mots-clés :
[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 neoformansRésumé
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
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