Synthesis, structure, and biological activity of novel bispidine derivatives
Malmakova A.Ye. Yu V.K. Praliyev K.D. Kaldybayeva A.B. Amirkulova M.K.
2021Innovare Academics Sciences Pvt. Ltd
International Journal of Applied Pharmaceutics
2021#13Issue special issue 169 - 74 pp.
Objective: Derivatives of 3,7-diazabicyclo[3.3.1]nonan-9-one attract considerable attention from pharmacists for the treatment of a wide range of diseases. According to this interest, the novel derivatives of 3-cyclopropanmethyl-7-alkoxyalkyl-3,7-diazabicyclo[3.3.1]nonan-9-one with isopropoxypropyl and ethoxypropyl substituents in the position 7 had been synthesized to study their biological activity and toxicity. The practical significance of the work is in the accumulation and development of scientific representations about diazabicyclic compounds, methods for their synthesis, structure, and properties, which can subsequently be used in a targeted design and identification of even more complex systems, as well as in the development of further research in the field of 3,7-diazabicyclo[3.3.1]nonanes. For this purpose, complexes of the synthesized compounds with β-cyclodextrin are obtained and their biological activity is investigated at the Department of Pharmacology of S.D. Asfendiyarov Kazakh National Medical University with the aid of the pharmacological tests. Methods: An experimental study of local anesthetic activity on the models of infiltration, conduction anesthesia, and acute toxicity of synthesized molecules was carried out using primary screening methods. Results: As a result of pharmacological screening, it has been found that the compounds exhibit local anesthetic activity and low toxicity and was recommended for in-depth study of their pharmacological properties. Conclusion: It turned out that a nature of the N-alkoxyalkyl radical does not affect the toxicity of cyclopropanmethyl-substituted bispidines. In the series of O-benzoyloximes of bispidinones, the isopropoxypropyl-substituted analog is 1.3 times less toxic than ethoxypropyl-one.
Activity , Acute toxicity , Anesthetics , Bispidine , Structure , Synthesis
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Department of of Physiologically Active Substances, A.B. Bekturov Institute of Chemical Sciences/Laboratory of Synthetic and Natural Medicinal Compounds Chemistry, Almaty, Kazakhstan
Department of Chemistry, Kazakh National Women’s Teacher Training University, Faculty of Natural Science, Almaty, Kazakhstan
Department of Pharmacology, Asfendiyarov Kazakh National Medical University, School of General Medicine, Almaty, Kazakhstan
Department of of Physiologically Active Substances
Department of Chemistry
Department of Pharmacology
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