Registration Number
0221U106840,
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
21-12-2021
Organization
Danylo Halytsky Lviv National Medical University
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The synthesis of "drug-like molecules" was performed by structural modification of the thiazolidinone moiety at position C-5, including its conjugation with known "biophore" heterocyclic systems, in particular the indole and pyrazole. On the basis of the logic-structural approach, the optimal directions of structural modification of 1-(2-amino-4-methylthiazol-5-yl)-ethanone under the aldol condensation reactions were performed. In order to diversify the library of isothiochromenothiazoles, alkylation of obtained via Knovenagel-hetero-Diels-Alder-domino reaction isothiochromeno[4a,4-d][1,3]thiazole with chloroacetamides was performed and the corresponding N-substituted derivatives were synthesized. Hybrid molecules based on isothiochromeno[4a,4-d[1,3]thiazole with isatin and indolecarboxylic fragments in the structure were obtained on the basis of ethyl ester and isothiochromenothiazole hydrazide. For the first time, a group of 3-arylidene(heteryrylidene)-1-(2-amino-4-methylthiazol-5-yl)ethanones not described in the literature was obtained based on the Kleisen-Schmidt reaction with various aldehydes. 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 V.
Finiuk Nataliia S.
Yushyn Ihor M.
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2021-12-21
