Tolperisone-based ionic liquids: synthesis and biological evaluation
Yelizaveta BELYANKOVA1, Anuar DAULETBAKOV1, Saniya TURSYNBEK1, Inkar MAKSOT1, Dariya ZOLOTAREVA1, Alexey ZAZYBIN1
1Kazakh British Technical University, Almaty, Kazakhstan
Tolperisone-based ionic liquids were synthesized by N-alkylation reaction of tolperisone free base (which was obtained by neutralization of commercially available hydrochloride) and corresponding halogen derivatives using acetonitrile as medium in classical (thermal activation) and alternative (ultrasound and/or microwave irradiation) conditions. The synthesized compounds were purified by ?ryst?ll?z?t??n from ???ro?r??t? solvent and then characterized by IR and NMR spectroscopy.
The application of the alternative methods is more effective in terms of reducing the exposure time and increasing the chemical efficiency compared to conventional conditions. Microwave-assisted method was found as effective way to promote synthesis in terms of reaction time and product yield.
Antimicrobial, antifungal, muelostimulating, antidiabetic, plant-growth stimulating activities and local anaestetic toxicity of synthesized ionic liquids were studied. Ionic liquids showed low or no toxicity toward toward E.coli, S. typhimurium, B.subtilis, S. aureus, P. aeruginosa, C.albicans. N-propyl tolperisone derivative showed good sorghum growth-stimulating activity and radioprotective properties. Based on the current data of biological activity of tolperisone's derivatives, it could be also concluded that myelostimulating activity decrease and anaesthetic toxicity increase with the growth of alkyl chain length.
This Research has been funded by the Science Committee of the Ministry of Education and Science of the Republic of Kazakhstan [AP19578051].