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Information × Registration Number 0220U100004, 0118U100275 , R & D reports Title Purposeful modification of the natural platform of betulonic acid for creation of the new biologically active compounds and materials. popup.stage_title Head Murlykina Maryna V., Кандидат хімічних наук Registration Date 02-01-2020 Organization State Scientific Institution "Institute for Single Crystals" of National Academy of Sciences of Ukraine popup.description2  The aim of the study is the creation of new compounds and materials for pharmaceutical use by means of purposeful modification of the natural triterpenoid – betulonic acid in the click-processes and reactions with formation of peptidomimetics. The aim of the second stage of the project is modification of betulonic acid in click-processes and reactions leading to peptidomimetics. While working on the second stage of the project (January-December 2019) the following results were obtained. A) The series of new chloro- and azido-derivatives of peptidomimetics on the basis of four-component Ugi reaction between 3-amino-5-methylisoxazole/3-aminothiophene-2-carboxylate, aromatic aldehydes, chloroacetic acid and isocyanides were synthetized. B) Selective methods for acylation of spiropyrrolidine-3,2'-oxindoles got in 1,3-dipolar cycloaddition reaction of isatins, acyclic α-amino acids and maleimide derivatives were elaborated and new non-planar heterocyclic azides were got on their basis. C) The series of new hybrid-molecules consisting of natural lupane core and synthetic pharmacophore fragments of spiropyrrolidine-3,2'-oxindoles/peptidomimetics on the basis of 3-amino-5-methylisoxazole and 3-aminothiophene-2-carboxylate were designed and synthetized. D) The antibacterial properties of newly created hybrid-molecules were studied in vitro using several reference strains of bacteria (B. Subtilis, E. Coli, S. Aureus, Ps. Aeruginosa). Product Description popup.authors popup.nrat_date 2020-04-02 Close