LAPPACONITINE MODIFICATIONS BY MULTICOMPONENT REACTIONS FOR PREPARATION OF PHARMACOLOGICALLY PROMISING AGENTS

Abstract

Diterpene alkaloids, which have a wide spectrum of physiological activity, considered as basic structures for such transformations [1, 2]. The availability of lappaconitine 1 have determined and caused interest in synthesizing new derivatives with reduced toxicity and enhanced pharmacological properties. The report summarizes the results of our research on the transformation of lappaconitine, which allowed for the introduction of additional heterocyclic pharmacophoric substituents into the aromatic fragment [3,4,5], as well as modifications of N-deethyllappaconitine with the introduction of propynyl substituents onto the nitrogen atom of the diterpene skeleton.

References

1. E. M. Tsyrlina, Sh. Sh. Sagdullaev, M. S. Yunusov. (2024). Synthetic Transformations of Lappaconitine.Chemistry of Natural Compounds.[Crossref]
2. X-Y. Liu, B-W. Ke, Y. Qin, F-P. Wang. The alkaloids: chemistry and biology, 87, 2022, 1.
3. Kirill Cheremnykh, Arkadiy Bryzgalov, Dmitry Baev, Sergey Borisov, Yulia Sotnikova, Victor Savelyev, Tatyana Tolstikova, Shamansur Sagdullaev, Elvira Shults. (2023). Synthesis, Pharmacological Evaluation, and Molecular Modeling of Lappaconitine–1,5-Benzodiazepine Hybrids.Molecules.[Crossref]
4. Kirill P. Cheremnykh, Victor A. Savelyev, Elvira E. Shults. (2021). An Efficient Access to 3,5‐Disubstituted Isoxazoles with Anthranilate Ester Moiety: Alkaloid Lappaconitine – Aryl Conjugates with an Isoxazole Linker.Asian Journal of Organic Chemistry.[Crossref]
5. K.P. Cheremnykh, V.A. Savelyev, S.A. Borisov, I.D. Ivanov, D.S. Baev, T.G. Tolstikova, V.A. Vavilin, E.E. Shults. Molecules 2020, 25, 5578.

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