Havrylyuk D. Synthesis, transformation and biological activity of new spirane and non-fused bicyclic derivatives on the base of 4-thiazolidones

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0407U002510

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

25-05-2007

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

Object - reactions of spiro-condensation and [2+3]-cyclocondensation in synthesis of 4-thiazolidones, interaction of thiazolidines with oxocompounds; the purpose - synthesis of new spirane and non-fused bicyclic substances based on the group of thiazolidine and search of effective and low-toxic physiologically active substances among them with anticancer, antimicrobial, antifungal and antituberculosis actions; methods - organic synthesis, NMR-, LC-MS- spectroscopies, traditional pharmacological screening QSAR-analysis; novelty - the effective methods of synthesis and transformation of spirane and non-fused bicyclic thiazolidine derivatives have been worked out. Biological activity of synthesized compounds have been studied, "structure-activity" correlations have been carried out; the outcomes - the row of new perspective and low-toxic compounds, which possess anticancer, antimicrobial, antifungal and tuberculostatic action has been identified, the recommendations regarding rational antimicrobial agentsdesign among the group of benzoxazinepyrazoline-substituted thiazolidones were proposed based on QSAR-analysis and docking studies; there are introduced into scientific and educational process of National Pharmaceutical University and National University "Lviv Politechnic"; area - pharmacy.

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