Danylchenko S. Synthesis, chemical transformation and biological activity of [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one derivatives.

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0417U002709

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

03-07-2017

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

The methods of synthesis of systematic series of derivatives [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones have been investigated in thesis. The structure of the compounds synthesized has been proven by elemental analysis and 1H NMR spectroscopy data. Computer prediction of the biological properties of derivatives [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones allowed to predict the most probable profile of biological activities of the compounds and their rate of acute toxicity. Biological screening confirmed the presence of antimicrobial activity and the absence of cytotoxic action of representatives [1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones derivatives. The substance 4-benzyl-1-{4-[4-(4-methoxyphenyl)piperazin-1-yl]-4-oxobutyl}[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one is recommended as a promising antimalarial agent for in-depth pharmacological study, to which the quality control methods is developed.

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