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Information × 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 popup.stage_title Head Lesyk Roman B., Доктор фармацевтичних наук Registration Date 30-11-2023 Organization Danylo Halytsky Lviv National Medical University popup.description2 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 popup.authors Konechnyi Yulian Tarasovych Kryshchyshyn-Dylevych Anna Lozynskyi Andrii V. Senkiv Yuliya V. Finiuk Nataliya Stepanivna Yushyn Ihor Mykhailovych popup.nrat_date 2023-11-30 Close