Registration Number
0222U000126,
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
03-01-2022
Organization
Danylo Halytsky Lviv National Medical University
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The synthesis of "drug-like molecules" based on condensed thiazolothiopyran derivatives, which was obtained by the reaction of hetero-Diels-Alder with dienophiles, which are effective reagents in pericyclic reactions, especially in the construction of various polycyclic systems. Based on the hybrid pharmacophore approach, the optimal directions for the production of thiazolopyridines were selected, namely the library of 5-methyl (arylidene) -7-phenyl-3H-thiazolo [4,5-b] pyridin-2-ones and further study of their pharmacological profile and toximetric parameters. In order to form heterocyclic combinatorial libraries, new condensed derivatives with a isothiocoumarin framework were synthesized by alkaline hydrolysis of 5-arylidene rhodanines through a two-step reaction in which intermediate hydrolysis products (thiopyruvic acids) formate heterocyclo-1 3-carboxylic acids, which became precursors for the production of the corresponding 1-oxo-1H-2-benzothiopyran-3-carboxylic acid chlorides. On the basis of the above-mentioned acid chlorides, for the first time, a group of functional derivatives of isothiocoumarin-3-carboxylic acids not described in the literature by the carboxyl group was obtained. The structure of the synthesized compounds was confirmed by complex NMR spectroscopy, elemental analysis and other spectral studies. Screening studies of the pharmacological activity of the synthesized condensed molecules allowed to identify a number of promising agents with anticancer and antimicrobial activities, on the basis of which the regularities of the «structure-action» correlation were established.
Product Description
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Konechnyi Yulian Tarasovych
Kryshchyshyn-Dylevych Anna Petrivna
Lozynskyi Andrii Volodymyrovych
Senkiv Yuliya V.
Finiuk Nataliya S.
Yushyn Ihor Mykhailovych
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2022-03-09
