Demchuk I. Synthesis, transformation and biological activity of esters and amides of rhodanine-3-carboxylic acids

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0411U000377

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

21-01-2011

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

Object - reactions of acylation, condensation, dimerization and heterocyclization for synthesis of target rows of 4-thiazolidinones and [5,5']-bithiazolidinones acids esters and amides; aim - synthesis of new derivatives of 2-thioxo-4-thiazolidinone-3-alkanecarboxylic acids, their bicyclic analogues and search of effective and low-toxic agents with antimicrobial, antifungal antiexudative and anticancer activities among them; methods - organic synthesis, mass-spectrometry, UV, IR- and NMR-spectroscopies, elemental analysis, pharmacological screening, SAR-analysis; novelty - the effective methods of synthesis and chemical modification of 4-thiazolidinones and [5,5']-bithiazolidinones acids have been worked out and optimized, biological activity of synthesized compounds have been studied and "structure-activity" correlations have been carried out; the outcomes - the row of new highly-active and low-toxic compounds, possessing antimicrobial, antifungal antiexudative and anticancer activities has been identified, the structural fragment as potential pharmacophores have been proposed based on SAR-analysis, that can be used for future optimisation of lead-compounds structures; these were introduced into scientific and educational process of Zaporizzhia State Medical University, Institute of Bioorganic Chemistry and Petrochemistry National Academy of Science of Ukraine, National Pharmaceutical University, National University "Lviv Politechnic", Ivan Franko Lviv National University; area - pharmacy.

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