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Information × Registration Number 0224U002772, 0121U100690 , R & D reports Title Molecular design, synthesis and biological activity evaluation of thiazolidinones and their derivatives as potential drug-like molecules popup.stage_title Head Lesyk Roman B., д.фарм.н. Registration Date 29-02-2024 Organization Danylo Halytsky Lviv National Medical University popup.description2  Optimal approaches to the synthesis of thiazole-pyridine hybrid molecules were developed using 1-[4-methyl-2-(2-pyridylamino)thiazol-5-yl]ethanone, which was obtained under the conditions of the [2+3]-cyclocondensation reaction of 1-(pyridine -2-yl)thiourea as an S,N-binucleophile and 2-chloroacetylacetone as an equivalent of the dielectrophilic synthon [C2]2+. Subsequently, the derivative (E)-3-(2-fluorophenyl)-1-[4-methyl-2-(2-pyridylamino)-thiazol-5-yl]-2-propen-1-one was synthesized starting from derivative 1 -[4-methyl-2-(2-pyridylamino)thiazol-5-yl]ethanone and 2-fluorobenzaldehyde under the conditions of the Claisen-Schmidt reaction. The next synthetic stage was based on transformations of the "enone" fragment of the synthesized compounds. It is also proposed to obtain high-yield Michael addition products by refluxing 1-[4-methyl-2-(2-pyridylamino)thiazol-5-yl]ethanone and 4-(2-mercaptoacetylamino)benzoic acid ethyl ether using N-methylpiperidine as a catalyst. Conducted screening studies of the pharmacological activity of synthesized thiazole-pyridine hybrid molecules and derivatives based on thiopyranothiazole made it possible to identify a number of promising agents with antineoplastic, antiviral, and antituberculosis activity, as well as to establish some "structure-activity" relationship. Product Description popup.authors Lozynskyi Andrii V. Roman Oleksandra M. Sementsiv Hryhorii M. Yushyn Ihor M. popup.nrat_date 2024-02-29 Close