Registration Number
0223U004704,
(0120U104782)
, R & D reports
Title
Thiazolidinones with polypharmacological properties: molecular design, synthesis and mechanisms of action of anticancer, anti-inflammatory and antimicrobial agents
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Підготовчий етап. Експериментальний етап (синтез похідних 4-тіазолідинону на основі гібрид фармакофорного підходу, синтез похідних роданін-3-карбонових кислот та синтез функціонально-заміщених похідних тіазолідинону, дослідження їх цитотоксичної/протизапальної/антимікробної активності та поглиблене дослідження механізмів реалізації біологічної активності). Підбиття підсумків досліджень етапу проєкту.
Head
Lesyk Roman B., Доктор фармацевтичних наук
Registration Date
30-11-2023
Organization
Danylo Halytsky Lviv National Medical University
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The aim of the project is to develop a methodology and approaches to the rational design of lead-compounds from the group of thiazolidinones and their functional derivatives as precursors of innovative drugs.
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As a result of the work, it was shown that when interacting with 4-thiazolidinethiones (iso- and thiorhodanine derivatives), it allows to implement various directions of synthetic research. Thus, the interaction of isorhodanine and 3-methyl-1H-pyrazol-5-amine produces 4-[(3-methyl-1H-pyrazol-5-yl)amino]-5H-thiazol-2-one, which is an effective methylene-active reagent to carry out the Kniovenagel reaction, which allows to obtain a series of 5-substituted derivatives. Systemic approaches to the design of biologically active 5-pyrazolylmethylene-4-thiazolidinones were proposed, which consisted in the Kniovenagel reaction of 1,3-diphenylpyrazole- and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehydes with 4-thiazolidinones , interactions of 5-ethoxy-4-thiazolidinones with 5-methyl-2-phenyl-2,4-dihydropyrazol-3-one and 4-dimethylaminomethylene-5-methyl-2-phenyl-2,4-dihydropyrazol-3-one with 2-thioxo-4-thiazolidinone. These approaches can be used alternatively depending on the task and the properties of individual reagents. It was established that the interaction of 5-methyl-2-phenyl-2,4-dihydropyrazol-3-one with triethyl orthoformate, regardless of temperature, proceeds with the formation of 4-((5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4 -yl)methyl)-3-methyl-1-phenyl-1H-pyrazolin-5-one, and not the expected 4-ethoxymethylene deriv.
Screening of the pharmacological activity of the synthesized molecules made it possible to investigate the in vivo toxicity and therapeutic efficacy
Product Description
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Konechnyi Yulian Tarasovych
Kryshchyshyn-Dylevych Anna
Lozynskyi Andrii V.
Senkiv Yuliya V.
Finiuk Nataliya Stepanivna
Yushyn Ihor Mykhailovych
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2023-11-30
