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
Highlights
Фармацевтичні наукиThe 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
The infection treatment was actual task of medicine both ancient and modern times
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
Summary
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. For the first time conducted antimicrobial screening of novel [1,2,4]triazolo[4,3-a]quinazolin5(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 sulfurcarbon chain possess antimicrobial activity against Acinetobacter baumannii or fungi Cryptococcus neoformans 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. Масив 169 нових похідних [1,2,4]триазоло[4,3-a]хіназолін-5(4H)-ону було тестовано на активність проти 5 видів бактерій: Escherihia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa та Staphylococcus aureus, та 2 видів грибів: Candida albicans та Cryptococcus neoformans. Проведене вперше тестування на антимікробну активність [1,2,4]триазоло[4,3-a]хіназолін5(4H)-онів показало, що сполуки, що не мають амідної групи, не проявляють антимікробної дії, проте деякі [1,2,4]триазоло[4,3-a]хіназолін-5(4H)-они, що містять амідну групу, приєднану за допомогою карбонового, або сульфур-карбонового ланцюгу, мають антимікробну активність проти Acinetobacter baumannii або Cryptococcus neoformans Ключові слова: [1,2,4]триазоло[4,3-a]хіназолін-5(4H)-он, антимікробна активність, Escherihia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Cryptococcus neoformans
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