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Information × Registration Number 0224U033555, (0124U002578) , R & D reports Title Development of new anesthetic agents popup.stage_title Розробка синтетичних підходів до нових аналогів бупівакаїну. Розробка методів синтезу нових аналогів бупівакаїну Head Mykhailiuk Pavlo K., Доктор хімічних наук Registration Date 30-12-2024 Organization Taras Shevchenko National University of Kyiv popup.description1 It is planned to: (a) synthesize new cyclic α-amino acids - analogues of pipecolic acid; (b) incorporate them into the bupivacaine structure; (c) establish the dependence of the action time on the structure of the 3D Fsp3-enriched bioisoster of piperidine in anesthetics; (e) to obtain new anesthetic agents with different strength and duration of action. popup.description2 Recent trends in drug discovery significantly changed the structural requirements for bioactive compounds. In this context chemists are currently looking for novel three-dimensionally (3D) shaped Fsp3-rich building blocks. In this project, we plan to (a) synthesize novel cyclic α-amino acids – analogues of pipecolic acid; (b) incorporate them into Bupivacaine structure; (c) establish the dependence of time of action on the structure of 3D Fsp3-rich bioisosteres of piperidine in the anesthetics; (d) obtaining novel anesthetic agents with different potency and time of action. Main tasks of the project: Planning a strategy for finding synthetic approaches to novel three-dimensionally (3D) shaped Fsp3-rich piperidine bioisosteres. Search for opportunities to create effective preparative methods for the synthesis of novel cyclic α-amino acids. Planning a strategy for finding synthetic approaches to novel anesthetics. Search for opportunities to create effective preparative methods for the synthesis of novel anesthetic agents. Evaluation of the effectiveness of novel anesthetic agents in the first approximation. Obtaining novel anesthetic agents with different duration of anesthetic action. Our studies, which served as the basis for this project, showed that the introduction of three-dimensionally shaped Fsp3-rich bioisosters of piperidine into the composition of Bupivacaine not only improves lipophilicity and water solubility, but also affects the duration of its anesthetic action, making it more predictable. To date, no one has tried to establish the dependence of the duration of anesthetic action on the structure of 3D Fsp3-rich bioisostere of piperidine in the anesthetic. The establishment of such a dependence requires the synthesis of new cyclic α-amino acids - analogs of pipecolic acid, which in turn requires the development of new synthetic approaches to the creation of such structures.  Product Description popup.authors Yehorova Tetiana V. Kyrychok Oleksandr O. popup.nrat_date 2024-12-30 Close