Registration Number
0223U002205,
0122U001809
, R & D reports
Title
Molecular design of bioisosters of natural compounds and multicomponent materials for targeted drug delivery
popup.stage_title
Head
Volovenko Yulian М., Доктор хімічних наук
Registration Date
12-02-2023
Organization
Taras Shevchenko National University of Kyiv
popup.description2
Research object - Heterocyclic biologically active compounds, including bioisosteres of natural compounds, and multicomponent systems based on biologically active substances for the needs of medical chemistry.
The purpose of the work is to create libraries of functionalized sp3-enriched five- and six-membered sultams and sultones, to determine their physical and chemical properties (in particular, solubility in water, lyophilicity, etc.) and biological activity. Creation of nanocomposites of the composition smait-polymer-small molecule in order to improve the pharmacological profile of biologically active agents. Testing for biological activity of the obtained compounds and composites.
Research methods - gel permeation chromatography, dynamic light scattering, NMR-, Mass-, UV- and IR-spectroscopy, determination of melting point, thin-layer chromatography, elemental analysis, in vitro and in vivo testing.
Methods for the synthesis of bioisosteres of natural biologically active compounds and a method for obtaining biocompatible water-soluble systems with an active component - smart polymer for targeted delivery to biological targets have been developed.
For the first time, bioisosteres of pyroglutamic acid were obtained by the intramolecular carbo-Michael cyclization strategy. The established regularities will allow to effectively introduce pharmacophoric groups and linkers into the structure of active components. Methods of obtaining biocompatible and water-soluble active component systems - smart polymer have also been developed. Such systems make it possible to significantly increase the solubility of active components in water, increase their biological activity and selectivity.
It was established that the synthesized D-PAA, D-PAA-an and DS-PAA copolymers do not show their own cytotoxicity against bacterial cells and prostate cancer cells, therefore they can be used as biocompatible matrices for the targeted delivery of sulfonamide derivatives and sultones.
Product Description
popup.authors
Bezugla Tetyana M.
Virych Pavlo A.
Vashchenko Bohdan V.
Dobrydnev Olexey V.
Kuziv Yuliya I.
Lampeka Rostyslav D.
Popova Mariia V.
Chumachenko Vasyl A.
popup.nrat_date
2023-02-12
