Registration Number
0221U101217,
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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Head
Lesyk Roman B., Доктор фармацевтичних наук
Registration Date
18-01-2021
Organization
Danylo Halytsky Lviv National Medical University
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Synthesis of drug-like molecules was performed by conjugation of 4-thiazolidinone or thiazole moieties with known "biophore" heterocyclic systems, in particular the pyridine, pyrazole and indole, which allows to preserve the pharmacological profile of these compounds and to analyze the structure-activity relationship. On the basis of logic-structural approach, the optimal directions of synthesis and structural modification of the target compounds were performed under reactions of [3+3]/[2+3]-cyclocondensation and Knoevenagel condensation. The sub-library of 5-arylidene-4-thiazolidinones, thiazolo [4,5-b] pyridines and thiazolo-indole-pyrazole conjugates was designed and synthesized. 2-Thioxothiazolidin-2-one derivatives have been shown to be effective reagents in reactions with an heterocyclic aldehydes in acetic acid medium providing to various 5-heterolylidene-rhodanine-3-carboxylic acids. The using of the [3+3]-cyclocondensation reaction of 4-amino-5H-thiazol-2-one with arylidenepyruvic and α, β-unsaturated ketones is an effective method for the synthesis of novel thiazolo[4,5-b]pyridine derivatives. Conducted screening studies of the pharmacological activity of the synthesized compounds allowed to identify a number of promising agents with antimicrobial and antitumor activities, as well as to establish some patterns of correlation "structure-activity" relationship.
Product Description
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Konechnyi Yulian T
Kryshchyshyn-Dylevych Anna P.
Lozynskyi Andrii V.
Senkiv Yuliya Vasylivna
Finiuk Nataliia S
Yushyn Ihor M.
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2021-01-18
