Kaminskyy D. Synthesis, transformation and biological activity of 4-azolidone-3-alkanecarboxylic acids

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0409U002908

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

05-06-2009

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

Object - reactions of [2+3]-cyclocondensation in synthesis of 4-thiazolidones, interaction of 4-azolidone-3-alkanecarboxylic acids with oxocompounds, reaction of heterocyclization, alkylation, acylation, cianoethylation; aim - synthesis, transformation and biological activity study of 4-azolidone-3-alkanecarboxylic acids and their derivatives as prototypes of innovative drugs with antitumor, antimycobacterial, anticonvulsant and antiviral actions ; methods - traditional and microwave organic synthesis, spectral analysis methods (NMR-, mass-, chromass-spectroscopies), thinlair and column chromatography, elemental analysis, traditional and high-throughput pharmacological screening, docking, QSAR-analysis; novelty - the effective new methods of synthesis and chemical modification for 4-azolidone-3-alkanecarboxylic acids have been worked out, biological activity of synthesized compounds have been studied and "structure-activity" correlations have been carried out; the outcomes - the row of new perspective highly-active compounds, possessing antitumor, antimycobacterial and antiviral activities has been identified, recommendations for rational design of potential antitumor agents have been proposed based on obtaining data, docking and QSAR-analysis; thee were introduced into scientific and educational process of National Pharmaceutical University, Zaporizzhia State Medical University and the program of course "Computer technologies in pharmacy" of Danylo Halytsky LNMU; area - pharmacy.

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