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

ScienceRise

Svitlana Danylchenko¹  Oleksandr Drushlyak²  Svitlana Kovalenko²  Alysha Elliott³  Johannes Zuegg³  Sergiy Kovalenko⁴ 

[1] National University of Pharmacy53 Pushkinska str., Kharkiv, Ukraine, 61002;National University of Pharmacy53 Pushkinska str., Kharkov, Ukraine, 61002;The Univercity of QueenslandBrisbane QLD 4072 Australia;V. N. Karazin Kharkiv National University4 Svobody squ., Kharkiv, Ukraine, 61022;

关键词: [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;   

DOI  :  10.15587/2313-8416.2016.67685

来源: DOAJ

【 摘 要 】

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

【 授权许可】

Unknown