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Information × Registration Number 0224U002730, 0120U100179 , R & D reports Title Chiral neurotropic compounds, ligands of CNS receptors. Synthesis, Structure, Structure-Property Relationship popup.stage_title Head Krysko Andrei A., Кандидат хімічних наук Registration Date 26-02-2024 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2 The purpose of the research: Establishing the pharmacological properties of the obtained compounds and screening according to the affinity of CNS benzodiazepine receptors. Synthesis of chiral 1,4-benzdiazepine derivatives containing reactive groups and their modification. Optically active 3-methyl-1,4-benzdiazepines were screened for their affinity to GABA of benzodiazepine receptors and it was established that in the above series of derivatives, S-isomers exhibit greater inhibitory properties compared to R-enantiomers. It was established that R-3-methyl-7-bromo-, S-3-methyl-7-chloro-5-(o-chlorophenyl)- and R-3-methyl-7-fluoro-1,4-benzdiazepines are not show a statistically significant effect on the behavioral indicators of animals in the "open field" test, S-3-methyl-7-bromo-5-(o-chlorophenyl)-1,4-benzdiazepine shows a pronounced depressant effect (sedative effect), which is dose-dependent , while S-3-methyl-7-fluoro-1,4-benzdiazepine not only did not have a sedative effect, but even had a certain activating effect at a low dose. The investigated compounds do not exhibit muscle relaxant effects and disturbances in the coordination of animal movements and differ in the magnitude of their anticonvulsant effect - R-3-methyl-7-bromo-1,4-benzdiazepine does not demonstrate anticonvulsant properties in the antagonism test with corazol, while R-3-methyl-7-bromo-5-(o-chlorophenyl)- and S-3-methyl-7-fluoro-1,4-benzdiazepines are the most active with an ED50 value of 0.057 μmol/kg. The anticonvulsant effect of R-3-methyl-7-bromo-5-(o-chlorophenyl)- and S-3-methyl-7-fluoro-1,4-benzdiazepines is close and is at the level of 0.4 μmol/kg. Chiral derivatives of 1,4-benzdiazepine containing a ester, carboxyl or amide functional group were synthesized. Product Description popup.authors Andronati Serhii A. Bachinsky Serhii Yu. Burenkova Nataliia O. Holovenko Mykola Ya. Kornilov Oleksandr Yu. Krysko Andrii А. Krysko Olha L. Larionov Vitalii B. Tsapenko Zhanna М. popup.nrat_date 2024-02-26 Close