SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF NOVEL BISPIDINE DERIVATIVES
Keywords:Bispidine, Synthesis, Structure, Activity, Anesthetics, Acute toxicity
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.
Bispidine-amino acid conjugates act as a novel scaffold for the design
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